Medicinal Chemistry and Pharmacognosy

Karl Werbovetz

Professor

Research Areas

Infectious Diseases,

Medicinal Chemistry & Pharmacognosy

werbovetz.1@osu.edu

(614) 292-5499

Professional Website

Parasitic diseases have a devastating effect on public health in developing areas of the world. Research in Karl Werbovetz’s group focuses on the discovery and development of new drug candidates against the protozoan parasitic diseases leishmaniasis, trypanosomiasis, and malaria, with most of our recent efforts concentrating on visceral leishmaniasis (VL) and human African trypanosomiasis (HAT).

1993 - PhD, University of Virginia, Chemistry

1988 - BS, State University of New York at Binghamton, Chemistry

Distinguished Teaching Award, 2005

<a href='https://www.mdpi.com/1420-3049/26/14/4213' target='_blank' class='bux-link'>Imidazoles as Potential Anticancer Agents: An Update on Recent Studies</a>, Molecules. 2021 Jul | journal-article. doi: 10.3390/molecules26144213.

<a href='' target='_blank' class='bux-link'>Synthesis and Antileishmanial Evaluation of Arylimidamide–Azole Hybrids Containing a Phenoxyalkyl Linker</a>, ACS Infectious Diseases. 2021 Feb | journal-article. doi: 10.1021/acsinfecdis.0c00855.

<a href='http://dx.doi.org/10.1016/j.bmcl.2019.126725' target='_blank' class='bux-link'>Synthesis and antileishmanial evaluation of thiazole orange analogs</a>, Bioorganic & Medicinal Chemistry Letters. 2020 Jan | journal-article. doi: 10.1016/j.bmcl.2019.126725.

<a href='' target='_blank' class='bux-link'>Microneedle-Based Delivery of Amphotericin B for Treatment of Cutaneous Leishmaniasis</a>, Biomedical Microdevices. 2019 Jan | journal-article. doi: 10.1007/s10544-018-0355-8.

<a href='' target='_blank' class='bux-link'>Antileishmanial Efficacy and Pharmacokinetics of DB766-Azole Combinations</a>, Antimicrobial Agents and Chemotherapy. 2018 Jan | journal-article. doi: 10.1128/aac.01129-17.

<a href='' target='_blank' class='bux-link'>Correction for Pandharkar et al., “Studies on the Antileishmanial Mechanism of Action of the Arylimidamide DB766: Azole Interactions and Role of CYP5122A1”</a>, Antimicrobial Agents and Chemotherapy. 2018 Jan | journal-article. doi: 10.1128/aac.01124-17.

<a href='' target='_blank' class='bux-link'>Synthesis and pharmacological evaluation of mono-arylimidamides as antileishmanial agents</a>, Bioorganic & Medicinal Chemistry Letters. 2016 May | journal-article. doi: 10.1016/j.bmcl.2016.03.082.

<a href='' target='_blank' class='bux-link'>Correction to Antileishmanial Activity of a Series of N2,N4-Disubstituted Quinazoline-2,4-diamines</a>, Journal of Medicinal Chemistry. 2016 Jan | journal-article. doi: 10.1021/acs.jmedchem.5b00981.

<a href='' target='_blank' class='bux-link'>Antileishmanial activity of some abietane diterpenoids from the cones of bald cypress, Taxodium distichum</a>, Planta Medica. 2014 Jul | journal-article. doi: 10.1055/s-0034-1382490.

<a href='' target='_blank' class='bux-link'>Studies on the Antileishmanial Mechanism of Action of the Arylimidamide DB766: Azole Interactions and Role of CYP5122A1</a>, Antimicrobial Agents and Chemotherapy. 2014 Jun | journal-article. doi: 10.1128/aac.02405-14.

<a href='' target='_blank' class='bux-link'>Antileishmanial Activity of a Series of N2,N4-Disubstituted Quinazoline-2,4-diamines</a>, Journal of Medicinal Chemistry. 2014 Jun | journal-article. doi: 10.1021/jm5000408.

<a href='' target='_blank' class='bux-link'>Evaluation of Antitrypanosomal Dihydroquinolines for Hepatotoxicity, Mutagenicity, and Methemoglobin Formation In Vitro</a>, International Journal of Toxicology. 2014 May | journal-article. doi: 10.1177/1091581814533971.

<a href='' target='_blank' class='bux-link'>Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives</a>, European Journal of Medicinal Chemistry. 2013 Sep | journal-article. doi: 10.1016/j.ejmech.2013.06.033.

<a href='' target='_blank' class='bux-link'>Discovery of benzamide analogs as negative allosteric modulators of human neuronal nicotinic receptors: Pharmacophore modeling and structure–activity relationship studies</a>, Bioorganic & Medicinal Chemistry. 2013 Aug | journal-article. doi: 10.1016/j.bmc.2013.03.082.

<a href='' target='_blank' class='bux-link'>Antileishmanial Activity of Some Abietane Diterpenoids from Taxodium distichum</a>, Planta Medica. 2013 Jul | journal-article. doi: 10.1055/s-0033-1348695.

<a href='' target='_blank' class='bux-link'>Synthesis and Antiprotozoal Activity of Dicationic m-Terphenyl and 1,3-Dipyridylbenzene Derivatives</a>, Journal of Medicinal Chemistry. 2013 Jun | journal-article. doi: 10.1021/jm400508e.

<a href='' target='_blank' class='bux-link'>Novel amidines and analogues as promising agents against intracellular parasites: a systematic review</a>, Parasitology. 2013 Apr | journal-article. doi: 10.1017/s0031182013000292.

<a href='' target='_blank' class='bux-link'>8,8-Dialkyldihydroberberines with Potent Antiprotozoal Activity</a>, Journal of Natural Products. 2012 Nov | journal-article. doi: 10.1021/np300638f.

<a href='' target='_blank' class='bux-link'>Antileishmanial bis-arylimidamides: DB766 analogs modified in the linker region and bis-arylimidamide structure–activity relationships</a>, Bioorganic & Medicinal Chemistry Letters. 2012 Nov | journal-article. doi: 10.1016/j.bmcl.2012.06.037.

<a href='' target='_blank' class='bux-link'>Synthesis, DNA binding and antileishmanial activity of low molecular weight bis-arylimidamides</a>, European Journal of Medicinal Chemistry. 2012 Sep | journal-article. doi: 10.1016/j.ejmech.2012.06.058.

<a href='' target='_blank' class='bux-link'>Induction of Oxidative Stress in Trypanosoma brucei by the Antitrypanosomal Dihydroquinoline OSU-40</a>, Antimicrobial Agents and Chemotherapy. 2012 Feb | journal-article. doi: 10.1128/aac.06386-11.

<a href='' target='_blank' class='bux-link'>Molecular factors governing inhibition of arylimidamides against Leishmania: Conservative computational modeling to improve chemotherapies</a>, Bioorganic & Medicinal Chemistry. 2011 Aug | journal-article. doi: 10.1016/j.bmc.2011.06.026.

<a href='' target='_blank' class='bux-link'>Correction to Synthesis and Antiprotozoal Activity of Cationic 1,4-Diphenyl-1H-1,2,3-triazoles</a>, Journal of Medicinal Chemistry. 2011 May | journal-article. doi: 10.1021/jm2005282.

<a href='' target='_blank' class='bux-link'>Potent antiprotozoal activity of a novel semi-synthetic berberine derivative</a>, Bioorganic & Medicinal Chemistry Letters. 2011 May | journal-article. doi: 10.1016/j.bmcl.2011.01.101.

<a href='' target='_blank' class='bux-link'>Structure-Activity Relationship Investigations Of Leishmanicidal N-Benzylcytisine Derivatives</a>, Chemical Biology & Drug Design. 2011 May | journal-article. doi: 10.1111/j.1747-0285.2011.01092.x.

<a href='' target='_blank' class='bux-link'>Antiparasitic Activity of C-Geranyl Flavonoids from Mimulus bigelovii</a>, Phytotherapy Research. 2011 Feb | journal-article. doi: 10.1002/ptr.3404.

<a href='' target='_blank' class='bux-link'>Simultaneous Determination of A Novel Antitrypanosomal Compound (OSU-36) and its Ester Derivative (OSU-40) in Plasma by HPLC: Application to First Pharmacokinetic Study in Rats</a>, Journal of Pharmacy & Pharmaceutical Sciences. 2011 Jan | journal-article. doi: 10.18433/j3cp4s.

<a href='' target='_blank' class='bux-link'>Identification of New Antileishmanial Leads from Hits Obtained by High-Throughput Screening</a>, Antimicrobial Agents and Chemotherapy. 2011 Jan | journal-article. doi: 10.1128/aac.05412-11.

<a href='' target='_blank' class='bux-link'>Synthesis and evaluation of oryzalin analogs against Toxoplasma gondii</a>, Bioorganic & Medicinal Chemistry Letters. 2010 Sep | journal-article. doi: 10.1016/j.bmcl.2010.07.003.

<a href='' target='_blank' class='bux-link'>New antileishmanial candidates and lead compounds</a>, Current Opinion in Chemical Biology. 2010 Aug | journal-article. doi: 10.1016/j.cbpa.2010.03.023.

<a href='' target='_blank' class='bux-link'>Dinitroaniline Activity in Toxoplasma gondii Expressing Wild-Type or Mutant α-Tubulin</a>, Antimicrobial Agents and Chemotherapy. 2010 Apr | journal-article. doi: 10.1128/aac.01150-09.

<a href='' target='_blank' class='bux-link'>Antitrypanosomal Activity of 1,2-Dihydroquinolin-6-ols and Their Ester Derivatives</a>, Journal of Medicinal Chemistry. 2010 Jan | journal-article. doi: 10.1021/jm900723w.

<a href='' target='_blank' class='bux-link'>A Novel Tropically Stable Oral Amphotericin B Formulation (iCo-010) Exhibits Efficacy against Visceral Leishmaniasis in a Murine Model</a>, PLoS Neglected Tropical Diseases. 2010 Jan | journal-article. doi: 10.1371/journal.pntd.0000913.

<a href='' target='_blank' class='bux-link'>Isolating Tubulin from Nonneural Sources</a>, Methods in Cell Biology. 2010 Jan | other. doi: 10.1016/s0091-679x(10)95002-4.

<a href='' target='_blank' class='bux-link'>α-Tubulin Mutations Alter Oryzalin Affinity and Microtubule Assembly Properties To Confer Dinitroaniline Resistance</a>, Eukaryotic Cell. 2010 Jan | journal-article. doi: 10.1128/ec.00140-10.

<a href='' target='_blank' class='bux-link'>Synthesis and Antiprotozoal Activity of Cationic 1,4-Diphenyl-1H-1,2,3-triazoles</a>, Journal of Medicinal Chemistry. 2009 Nov | journal-article. doi: 10.1021/jm901178d.

<a href='' target='_blank' class='bux-link'>Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes</a>, European Journal of Medicinal Chemistry. 2009 Sep | journal-article. doi: 10.1016/j.ejmech.2009.03.014.

<a href='' target='_blank' class='bux-link'>Synthesis and Antiprotozoal Properties of Pentamidine Congeners Bearing the Benzofuran Motif</a>, Journal of Medicinal Chemistry. 2009 Aug | journal-article. doi: 10.1021/jm9006406.

<a href='' target='_blank' class='bux-link'>Highly Effective Oral Amphotericin B Formulation against Murine Visceral Leishmaniasis</a>, The Journal of Infectious Diseases. 2009 Aug | journal-article. doi: 10.1086/600105.

<a href='' target='_blank' class='bux-link'>Synthesis and Antiprotozoal Activity of Pyridyl Analogues of Pentamidine</a>, Journal of Medicinal Chemistry. 2009 Jul | journal-article. doi: 10.1021/jm900805v.

<a href='' target='_blank' class='bux-link'>Structure−Activity Study of Pentamidine Analogues as Antiprotozoal Agents</a>, Journal of Medicinal Chemistry. 2009 Mar | journal-article. doi: 10.1021/jm801547t.

<a href='' target='_blank' class='bux-link'>Redox-active dinitrodiphenylthioethers against Leishmania: Synthesis, structure–activity relationships and mechanism of action studies</a>, Bioorganic & Medicinal Chemistry. 2009 Jan | journal-article. doi: 10.1016/j.bmc.2008.11.031.

<a href='' target='_blank' class='bux-link'>Visceral leishmaniasis affects liver and spleen concentrations of amphotericin B following administration to mice</a>, Journal of Antimicrobial Chemotherapy. 2009 Jan | journal-article. doi: 10.1093/jac/dkp465.

<a href='' target='_blank' class='bux-link'>Pharmacological and biological screening of ascorbigen: protection against glucose-induced endothelial cell toxicity</a>, Phytotherapy Research. 2008 Oct | journal-article. doi: 10.1002/ptr.2494.

<a href='' target='_blank' class='bux-link'>Synthesis and Antiprotozoal Activity of Cationic 2-Phenylbenzofurans</a>, Journal of Medicinal Chemistry. 2008 Oct | journal-article. doi: 10.1021/jm800918v.

<a href='' target='_blank' class='bux-link'>Antiparasitic activity of certain isoquinoline alkaloids and their hypothetical complexes with oligonucleotides</a>, Chemistry of Natural Compounds. 2008 Oct | journal-article. doi: 10.1007/s10600-008-9057-4.

<a href='' target='_blank' class='bux-link'>Inhibition by Dications of In Vitro Growth of Leishmania major and Leishmania tropica: Causative Agents of Old World Cutaneous Leishmaniasis</a>, Journal of Parasitology. 2008 Jun | journal-article. doi: 10.1645/ge-1387.1.

<a href='' target='_blank' class='bux-link'>Flavylium Salts as Precursors of Biologically Active Chalcones</a>, Letters in Drug Design & Discovery. 2008 Jan | journal-article. doi: 10.2174/157018008783406697.

<a href='' target='_blank' class='bux-link'>Azaterphenyl diamidines as antileishmanial agents</a>, Bioorganic & Medicinal Chemistry Letters. 2008 Jan | journal-article. doi: 10.1016/j.bmcl.2007.10.091.

<a href='' target='_blank' class='bux-link'>Inhibitors of Tubulin Assembly Identified through Screening a Compound Library</a>, Chemical Biology & Drug Design. 2008 Jan | journal-article. doi: 10.1111/j.1747-0285.2008.00729.x.

<a href='' target='_blank' class='bux-link'>Synthesis and in Vitro Antiprotozoal Activity of Bisbenzofuran Cations</a>, Journal of Medicinal Chemistry. 2007 Oct | journal-article. doi: 10.1021/jm0708634.

<a href='' target='_blank' class='bux-link'>Synthesis, biological evaluation, and molecular modeling of 3,5-substituted-N1-phenyl-N4,N4-di-n-butylsulfanilamides as antikinetoplastid antimicrotubule agents</a>, Bioorganic & Medicinal Chemistry. 2007 Sep | journal-article. doi: 10.1016/j.bmc.2007.06.042.

<a href='' target='_blank' class='bux-link'>Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes</a>, European Journal of Medicinal Chemistry. 2007 Apr | journal-article. doi: 10.1016/j.ejmech.2006.11.006.

<a href='' target='_blank' class='bux-link'>Antileishmanial and Antimalarial Chalcones: Synthesis, Efficacy and Cytotoxicity of Pyridinyl and Naphthalenyl Analogs</a>, Medicinal Chemistry. 2007 Mar | journal-article. doi: 10.2174/157340607780059530.

<a href='' target='_blank' class='bux-link'>Natural Products from Plants as Drug Candidates and Lead Compounds Against Leishmaniasis and Trypanosomiasis</a>, Current Medicinal Chemistry. 2006 Sep | journal-article. doi: 10.2174/092986706778201611.

<a href='' target='_blank' class='bux-link'>Antikinetoplastid antimitotic activity and metabolic stability of dinitroaniline sulfonamides and benzamides</a>, Bioorganic & Medicinal Chemistry. 2006 Aug | journal-article. doi: 10.1016/j.bmc.2006.04.017.

<a href='' target='_blank' class='bux-link'>Pre-systemic metabolism prevents in vivo antikinetoplastid activity of N1,N4-substituted 3,5-dinitro sulfanilamide, GB-II-150</a>, Life Sciences. 2006 Aug | journal-article. doi: 10.1016/j.lfs.2006.03.028.

<a href='' target='_blank' class='bux-link'>Activity of and Initial Mechanistic Studies on a Novel Antileishmanial Agent Identified through in Silico Pharmacophore Development and Database Searching</a>, Journal of Medicinal Chemistry. 2006 Jun | journal-article. doi: 10.1021/jm060156v.

<a href='' target='_blank' class='bux-link'>A thalidomide analogue with in vitro antiproliferative, antimitotic, and microtubule-stabilizing activities</a>, Molecular Cancer Therapeutics. 2006 Feb | journal-article. doi: 10.1158/1535-7163.mct-05-0254.

<a href='' target='_blank' class='bux-link'>Leishmania tarentolae: Purification and characterization of tubulin and its suitability for antileishmanial drug screening</a>, Experimental Parasitology. 2006 Jan | journal-article. doi: 10.1016/j.exppara.2006.04.008.

<a href='' target='_blank' class='bux-link'>Activity of Amidine-containing Diphenylureas Against P. falciparum</a>, Letters in Drug Design & Discovery. 2005 Mar | journal-article. doi: 10.2174/1570180053175061.

<a href='' target='_blank' class='bux-link'>Promising therapeutic targets for antileishmanial drugs</a>, Expert Opinion on Therapeutic Targets. 2005 Feb | journal-article. doi: 10.1517/14728222.6.4.407.

<a href='' target='_blank' class='bux-link'>Conformationally restricted analogs of Combretastatin A-4 derived from SU5416</a>, Bioorganic & Medicinal Chemistry Letters. 2005 Jan | journal-article. doi: 10.1016/j.bmcl.2005.09.001.

<a href='' target='_blank' class='bux-link'>Isoflavonoids and Other Compounds from Psorothamnus arborescens with Antiprotozoal Activities</a>, Journal of Natural Products. 2005 Jan | journal-article. doi: 10.1021/np0502600.

<a href='' target='_blank' class='bux-link'>Antikinetoplastid activity of 3-aryl-5-thiocyanatomethyl-1,2,4-oxadiazoles</a>, Bioorganic & Medicinal Chemistry. 2004 Jun | journal-article. doi: 10.1016/j.bmc.2004.03.054.

<a href='' target='_blank' class='bux-link'>Purification and identification of a fatty acyl-CoA synthetase from Trypanosoma brucei</a>, Molecular and Biochemical Parasitology. 2004 May | journal-article. doi: 10.1016/j.molbiopara.2004.01.003.

<a href='' target='_blank' class='bux-link'>SYNTHESIS OF DICATIONIC 2,5-DIARYLPYRROLES</a>, Heterocyclic Communications. 2004 Jan | journal-article. doi: 10.1515/hc.2004.10.6.423.

<a href='' target='_blank' class='bux-link'>Antiprotozoal Compounds from Psorothamnus polydenius</a>, Journal of Natural Products. 2004 Jan | journal-article. doi: 10.1021/np049682k.

<a href='' target='_blank' class='bux-link'>Selective Antimicrotubule Activity ofN1-Phenyl-3,5-dinitro-N4,N4-di-n-propylsulfanilamide (GB-II-5) against Kinetoplastid Parasites</a>, Molecular Pharmacology. 2003 Nov | journal-article. doi: 10.1124/mol.64.6.1325.

<a href='' target='_blank' class='bux-link'>Antiprotozoal activities of symmetrical bishydroxamic acids</a>, Bioorganic & Medicinal Chemistry. 2003 Oct | journal-article. doi: 10.1016/s0968-0896(03)00522-4.

<a href='' target='_blank' class='bux-link'>Antileishmanial dinitroaniline sulfonamides with activity against parasite tubulin</a>, Bioorganic & Medicinal Chemistry Letters. 2002 Sep | journal-article. doi: 10.1016/s0960-894x(02)00465-1.

<a href='' target='_blank' class='bux-link'>Antileishmanial Activities of Several Classes of Aromatic Dications</a>, Antimicrobial Agents and Chemotherapy. 2002 Mar | journal-article. doi: 10.1128/aac.46.3.797-807.2002.

<a href='' target='_blank' class='bux-link'>Tubulin as an Antiprotozoal Drug Target</a>, Mini-Reviews in Medicinal Chemistry. 2002 Jan | journal-article. doi: 10.2174/1389557023405648.

<a href='' target='_blank' class='bux-link'>Selective Lead Compounds against Kinetoplastid Tubulin</a>, Advances In Experimental Medicine And Biology. 1 Jan | other. doi: 10.1007/978-0-387-77570-8_4.

<a href='' target='_blank' class='bux-link'>Cellular effects of leishmanial tubulin inhibitors on L. donovani</a>, Molecular and Biochemical Parasitology. 2000 Oct | journal-article. doi: 10.1016/s0166-6851(00)00272-3.

<a href='' target='_blank' class='bux-link'>Target-Based Drug Discovery for Malaria, Leishmaniasis, and Trypanosomiasis</a>, Current Medicinal Chemistry. 2000 Aug | journal-article. doi: 10.2174/0929867003374615.

<a href='' target='_blank' class='bux-link'>Analysis of stereoelectronic properties of camptothecin analogues in relation to biological activity</a>, Bioorganic & Medicinal Chemistry. 2000 Jul | journal-article. doi: 10.1016/s0968-0896(00)00111-5.

<a href='' target='_blank' class='bux-link'>Purification, characterization, and drug susceptibility of tubulin from Leishmania</a>, Molecular and Biochemical Parasitology. 1999 Jan | journal-article. doi: 10.1016/s0166-6851(98)00146-7.

<a href='' target='_blank' class='bux-link'>Synthesis and Biological Evaluation of 4-Chloro-3,5-dinitrobenzotrifluoride Analogues as Antileishmanial Agents</a>, Journal of Medicinal Chemistry. 1998 Nov | journal-article. doi: 10.1021/jm9804073.

<a href='' target='_blank' class='bux-link'>Structure-activity relationship for DNA topoisomerase II-induced DNA cleavage by azatoxin analogues</a>, Bioorganic & Medicinal Chemistry. 1997 Sep | journal-article. doi: 10.1016/s0968-0896(97)00113-2.

<a href='' target='_blank' class='bux-link'>Glycosyl phosphatidylinositol myristoylation in African trypanosomes</a>, Molecular and Biochemical Parasitology. 1997 Mar | journal-article. doi: 10.1016/s0166-6851(96)02820-4.

<a href='' target='_blank' class='bux-link'>Trypanocidal analogs of myristate and myristoyllysophosphatidylcholine</a>, Molecular and Biochemical Parasitology. 1996 Oct | journal-article. doi: 10.1016/0166-6851(96)02708-9.

<a href='' target='_blank' class='bux-link'>Lipid metabolism in Trypanosoma brucei: utilization of myristate and myristoyllysophosphatidylcholine for myristoylation of glycosyl phosphatidylinositols</a>, Biochemical Journal. 1996 Sep | journal-article. doi: 10.1042/bj3180575.

<a href='' target='_blank' class='bux-link'>Inhibition of DNA Topoisomerase II by Azaelliptitoxins Functionalized in the Variable Substituent Domain</a>, Journal of Medicinal Chemistry. 1996 May | journal-article. doi: 10.1021/jm9508806.

<a href='' target='_blank' class='bux-link'>Myristate exchange on the Trypanosoma brucei variant surface glycoprotein.</a>, Proceedings of the National Academy of Sciences. 1996 Feb | journal-article. doi: 10.1073/pnas.93.3.1178.

<a href='' target='_blank' class='bux-link'>Toxicity of myristic acid analogs toward African trypanosomes.</a>, Proceedings of the National Academy of Sciences. 1994 Oct | journal-article. doi: 10.1073/pnas.91.21.9735.

<a href='' target='_blank' class='bux-link'>On the mechanism of arylamine-DNA adduct formation</a>, Bioorganic & Medicinal Chemistry Letters. 1994 Oct | journal-article. doi: 10.1016/0960-894x(94)85033-x.

<a href='' target='_blank' class='bux-link'>Cleavable complex formation in Leishmania chagasi treated with anilinoacridines</a>, Molecular and Biochemical Parasitology. 1994 May | journal-article. doi: 10.1016/0166-6851(94)90110-4.

<a href='' target='_blank' class='bux-link'>Cytotoxicity of acridine compounds for Leishmania promastigotes in vitro</a>, Antimicrobial Agents and Chemotherapy. 1992 Feb | journal-article. doi: 10.1128/aac.36.2.495.

<a href='' target='_blank' class='bux-link'>Treatment of leishmaniasis and trypanosomiasis</a>, Current Opinion in Infectious Diseases. 1992 Jan | journal-article. doi: 10.1097/00001432-199212000-00015.

<a href='' target='_blank' class='bux-link'>Tubulin binding of conformationally restricted bis-aryl compounds</a>, Bioorganic & Medicinal Chemistry Letters. 1991 Jan | journal-article. doi: 10.1016/s0960-894x(01)81034-9.

Yulin Ren

Research Scientist

Medicinal Chemistry and Pharmacognosy

Research Areas

Natural Products

ren.41@osu.edu

(740) 707-1263

• Chromatography supported isolation of the minor components from higher plants or other natural organisms.
• Spectroscopic aided structure determination of complex natural products.
• Synthetic modification of bioactive lead compounds.
• Single-crystal X-ray diffraction based determination of conformation and configuration of natural products with multiple chiral centers.
• Bioassay design, development, and performance to evaluate the bioactivities of natural products.

<a href='https://www.mdpi.com/1422-0067/23/23/14546' target='_blank' class='bux-link'>Effects of Corchorusoside C on NF-κB and PARP-1 Molecular Targets and Toxicity Profile in Zebrafish</a>, International Journal of Molecular Sciences. 2022 Nov | journal-article. doi: 10.3390/ijms232314546.

<a href='https://www.mdpi.com/1420-3049/26/18/5675' target='_blank' class='bux-link'>Interaction of (+)-Strebloside and Its Derivatives with Na+/K+-ATPase and Other Targets</a>, Molecules. 2021 Sep | journal-article. doi: 10.3390/molecules26185675.

<a href='https://www.mdpi.com/1420-3049/26/12/3672' target='_blank' class='bux-link'>Structural Insights into the Interactions of Digoxin and Na+/K+-ATPase and Other Targets for the Inhibition of Cancer Cell Proliferation</a>, Molecules. 2021 Jun | journal-article. doi: 10.3390/molecules26123672.

Liva Rakotondraibe

Associate Professor

Medicinal Chemistry and Pharmacognosy

Research Areas

Cancer,

Medicinal Chemistry & Pharmacognosy,

Natural Products

rakotondraibe.1@osu.edu

(614) 292-4733

Professional Website

New natural product sources (new and unidentified fungal and bacterial microorganisms, microbial endophytes, new endemic and medicinal plant species, etc.) contain many undiscovered potential bioactive secondary metabolites that can be used to combat world’s deadly diseases including cancer, malaria, viral infections, and chemoresistance. Their investigation must be prioritized in order to discover new pharmacophores for potential drug candidates. My lab focuses on (1) bioassay-guided isolation, structural elucidation and development of bioactive compounds from natural sources, (2) Drug discovery from Madagascan natural products and (3) drug discovery from ethnomedicine. One of our recent ongoing projects is on the development of insecticides that can be used to control mosquito vector of Zika virus from Madagascan endemic plants.

2003, PhD, Hiroshima University, Pharmaceutical Sciences (Medicinal Natural Product Chemistry

1998, DEA (Diplome d'Etude Approfondie), Equivalent to MS, Mention "Tres bien", University of Antananarivo, Organic Chemistry/ Natural Product Chemistry

Dean's Innovation Award, The Ohio State University College of Pharmacy, 2023

PRE President's Research Excellence Accelerator Award, 2022

JSPS-Bridge (Japanese Society for the Promotion of Science) Fellowship, 2017 - 2018

Postdoctoral Fellowship from the Japanese Society for the Promotion of Science (JSPS), 2005 - 2007

Japanese Government (Mombukagakusho): Ministry of Education, Culture, Sports, Science and Technology (MEXT), 1999 - 2003

<a href='http://dx.doi.org/10.1128/mbio.03284-22' target='_blank' class='bux-link'>Histoplasma capsulatum
requires peroxisomes for multiple virulence functions including siderophore biosynthesis</a>, mBio. 2023 Jul | journal-article. doi: 10.1128/mbio.03284-22.

<a href='http://dx.doi.org/10.1016/j.phytochem.2023.113638' target='_blank' class='bux-link'>Bioactive and unusual steroids from Penicillium fungi</a>, Phytochemistry. 2023 May | journal-article. doi: 10.1016/j.phytochem.2023.113638.

<a href='https://doi.org/10.1039/D2NP00080F' target='_blank' class='bux-link'>Strategies for the discovery of potential anticancer agents from plants collected from Southeast Asian tropical rainforests as a case study</a>, Natural Product Reports. 2023 Jan | journal-article. doi: 10.1039/D2NP00080F.

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<a href='' target='_blank' class='bux-link'>Antiproliferative Compounds fromPongamiopsis pervilleanafrom the Madagascar Dry Forest(1)</a>, Journal of Natural Products. 2010 Sep | journal-article. doi: 10.1021/np100430r.

<a href='' target='_blank' class='bux-link'>ChemInform Abstract: ent-Kaurane Diterpenoid Glycosides from the Leaves of Cussonia racemosa, a Malagasy Endemic Plant</a>, ChemInform. 2010 May | journal-article. doi: 10.1002/chin.200232177.

<a href='' target='_blank' class='bux-link'>New and Bioactive Natural Products Isolated from Madagascar Plants and Marine Organisms</a>, Current Medicinal Chemistry. 2010 Apr | journal-article. doi: 10.2174/092986710790827834.

<a href='' target='_blank' class='bux-link'>Secoiridoid and iridoid glucosides from the leaves of Fraxinus griffithii</a>, Journal of Natural Medicines. 2009 Aug | journal-article. doi: 10.1007/s11418-009-0354-4.

<a href='' target='_blank' class='bux-link'>ChemInform Abstract: Bryophytes: Bio- and Chemical Diversity, Bioactivity and Chemosystematics</a>, ChemInform. 2009 Apr | journal-article. doi: 10.1002/chin.200917258.

<a href='' target='_blank' class='bux-link'>Chemical constituents of Pteris cretica Linn. (Pteridaceae)</a>, Biochemical Systematics and Ecology. 2009 Apr | journal-article. doi: 10.1016/j.bse.2009.01.012.

<a href='' target='_blank' class='bux-link'>ChemInform Abstract: Marchantiophyta (Liverworts): Rich Sources of Macrocyclic Bis(bibenzyls)</a>, ChemInform. 2009 Feb | journal-article. doi: 10.1002/chin.200906239.

<a href='' target='_blank' class='bux-link'>Bryophytes: Bio- and Chemical Diversity, Bioactivity and Chemosystematics</a>, HETEROCYCLES. 2009 Jan | journal-article. doi: 10.3987/rev-08-sr(f)3.

<a href='' target='_blank' class='bux-link'>Chemical and biologically active constituents of Pteris multifida</a>, Journal of Natural Medicines. 2008 Jun | journal-article. doi: 10.1007/s11418-008-0265-9.

<a href='' target='_blank' class='bux-link'>Secondary Metabolites ofCinnamosma madagascariensisand Their α-Glucosidase Inhibitory Properties</a>, Journal of Natural Products. 2008 Jan | journal-article. doi: 10.1021/np070474c.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-58149149897&partnerID=MN8TOARS' target='_blank' class='bux-link'>Macaflavanones A-G, prenylated flavanones from the leaves of Macaranga tanarius</a>, Journal of Natural Products. 2008 Jan | journal-article. doi: 10.1021/np800380d.

<a href='' target='_blank' class='bux-link'>Marchantiophyta (Liverworts): Rich Sources of Macrocyclic Bis(bibenzyls)</a>, HETEROCYCLES. 2008 Jan | journal-article. doi: 10.3987/rev-08-sr(n)3.

<a href='' target='_blank' class='bux-link'>Chemical Constituents of Malagasy Liverworts. 6. A Myltaylane Caffeate with Nitric Oxide Inhibitory Activity fromBazzania nitida</a>, Journal of Natural Products. 2007 May | journal-article. doi: 10.1021/np060549x.

<a href='' target='_blank' class='bux-link'>Chemical Constituents of Malagasy Liverworts: Cyclomyltaylanoids from Bazzania madagassa. Part 4.</a>, ChemInform. 2007 Apr | journal-article. doi: 10.1002/chin.200715171.

<a href='' target='_blank' class='bux-link'>Cinnamacrins A−C, Cinnafragrin D, and Cytostatic Metabolites with α-Glucosidase Inhibitory Activity fromCinnamosma macrocarpa</a>, Journal of Natural Products. 2007 Feb | journal-article. doi: 10.1021/np060435l.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-34447550055&partnerID=MN8TOARS' target='_blank' class='bux-link'>Bioactive compounds from liverworts: Inhibition of lipopolysaccharide-induced inducible NOS mRNA in RAW 264.7 cells by Herbertenoids and Cuparenoids</a>, Phytomedicine. 2007 Jan | journal-article. doi: 10.1016/j.phymed.2006.09.011.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-61749086867&partnerID=MN8TOARS' target='_blank' class='bux-link'>Malagasy liverworts, sourcc of new and biologically active compounds</a>, Natural Product Communications. 2007 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33846124222&partnerID=MN8TOARS' target='_blank' class='bux-link'>Phytochemistry of three selected liverworts: Conocephalum conicum, Plagiochila barteri and P. terebrans</a>, Arkivoc. 2007 Jan | journal-article. .

<a href='' target='_blank' class='bux-link'>Cinnafragrins A−C, Dimeric and Trimeric Drimane Sesquiterpenoids fromCinnamosmafragrans, and Structure Revision of Capsicodendrin⊥</a>, Journal of Natural Products. 2006 Aug | journal-article. doi: 10.1021/np0601298.

<a href='' target='_blank' class='bux-link'>Essential oil composition of four Croton species from Madagascar and their chemotaxonomy</a>, Biochemical Systematics and Ecology. 2006 Aug | journal-article. doi: 10.1016/j.bse.2006.02.005.

<a href='' target='_blank' class='bux-link'>Inhibitory activity of nitric oxide production in RAW 264.7 cells of daldinals A–C from the fungus Daldinia childiae and other metabolites isolated from inedible mushrooms</a>, Journal of Natural Medicines. 2006 Aug | journal-article. doi: 10.1007/s11418-006-0010-1.

<a href='' target='_blank' class='bux-link'>An Acetylated Eudesmane Glucoside from Apodytes dimidiata Growing in Madagascar</a>, Zeitschrift für Naturforschung B. 2006 Jan | journal-article. doi: 10.1515/znb-2006-0123.

<a href='' target='_blank' class='bux-link'>Chemical Constituents of Malagasy Liverworts, Part V: Prenyl Bibenzyls and Clerodane Diterpenoids with Nitric Oxide Inhibitory Activity from Radula appressa and Thysananthus spathulistipus</a>, CHEMICAL & PHARMACEUTICAL BULLETIN. 2006 Jan | journal-article. doi: 10.1248/cpb.54.1046.

<a href='' target='_blank' class='bux-link'>Chemical Constituents of Malagasy Liverworts. Part 5. Prenyl Bibenzyls and Clerodane Diterpenoids with Nitric Oxide Inhibitory Activity from Radula appressa and Thysananthus spathulistipus.</a>, ChemInform. 2006 Jan | journal-article. doi: 10.1002/chin.200652191.

<a href='' target='_blank' class='bux-link'>Chemical constituents of Malagasy liverworts: Cyclomyltaylanoids from Bazzania madagassa</a>, Phytochemistry. 2006 Jan | journal-article. doi: 10.1016/j.phytochem.2006.06.001.

<a href='' target='_blank' class='bux-link'>Inhibition of Nitric Oxide Production in RAW 264.7 Cells by Azaphilones from Xylariaceous Fungi</a>, Biological & Pharmaceutical Bulletin. 2006 Jan | journal-article. doi: 10.1248/bpb.29.34.

<a href='' target='_blank' class='bux-link'>Momordica charantia Constituents and Antidiabetic Screening of the Isolated Major Compounds</a>, CHEMICAL & PHARMACEUTICAL BULLETIN. 2006 Jan | journal-article. doi: 10.1248/cpb.54.1017.

<a href='' target='_blank' class='bux-link'>Momordica charantia Constituents and Antidiabetic Screening of the Isolated Major Compounds.</a>, ChemInform. 2006 Jan | journal-article. doi: 10.1002/chin.200652188.

<a href='' target='_blank' class='bux-link'>Penicillium sclerotiorum Catalyzes the Conversion of Herbertenediol into Its Dimers: Mastigophorenes A and B.</a>, ChemInform. 2005 Jul | journal-article. doi: 10.1002/chin.200529193.

<a href='' target='_blank' class='bux-link'>Bis(bibenzyls) from Liverworts Inhibit Lipopolysaccharide-Induced Inducible NOS in RAW 264.7 Cells: A Study of Structure−Activity Relationships and Molecular Mechanism</a>, Journal of Natural Products. 2005 Jan | journal-article. doi: 10.1021/np0502589.

<a href='' target='_blank' class='bux-link'>Chemical Constituents of Malagasy Liverworts, Part III: Sesquiterpenoids from Bazzania decrescens and Bazzania madagassa</a>, CHEMICAL & PHARMACEUTICAL BULLETIN. 2005 Jan | journal-article. doi: 10.1248/cpb.53.515.

<a href='' target='_blank' class='bux-link'>Penicillium sclerotiorum Catalyzes the Conversion of Herbertenediol into Its Dimers: Mastigophorenes A and B</a>, CHEMICAL & PHARMACEUTICAL BULLETIN. 2005 Jan | journal-article. doi: 10.1248/cpb.53.256.

<a href='' target='_blank' class='bux-link'>Constituents of Isotachis aubertii (Isotachidaceae) collected in Madagascar</a>, Biochemical Systematics and Ecology. 2004 Nov | journal-article. doi: 10.1016/j.bse.2004.04.009.

<a href='' target='_blank' class='bux-link'>Chemical Constituents of Malagasy Liverworts, Part II: Mastigophoric Acid Methyl Ester of Biogenetic Interest from Mastigophora diclados (Lepicoleaceae Subf. Mastigophoroideae)</a>, CHEMICAL & PHARMACEUTICAL BULLETIN. 2004 Jan | journal-article. doi: 10.1248/cpb.52.1382.

<a href='' target='_blank' class='bux-link'>Cussosaponins A—E, Triterpene Saponins from the Leaves of Cussonia racemosa, a Malagasy Endemic Plant.</a>, ChemInform. 2003 Mar | journal-article. doi: 10.1002/chin.200309174.

<a href='' target='_blank' class='bux-link'>A New ent-Kaurane Diterpenoid Glycoside from the Leaves of Cussonia bojeri, a Malagasy Endemic Plant.</a>, ChemInform. 2003 Jan | journal-article. doi: 10.1002/chin.200303150.

<a href='' target='_blank' class='bux-link'>ent-Kaurane diterpenoid glycosides from a Malagasy endemic plant, Cussonia vantsilana</a>, Phytochemistry. 2002 Oct | journal-article. doi: 10.1016/s0031-9422(02)00263-7.

<a href='' target='_blank' class='bux-link'>Clerodane and labdane diterpene glycosides from a Malagasy endemic plant, Cussonia racemosa</a>, Phytochemistry. 2002 Jun | journal-article. doi: 10.1016/s0031-9422(02)00064-x.

<a href='' target='_blank' class='bux-link'>A New ent-Kaurane Diterpenoid Glycoside from the Leaves of Cussonia bojeri, a Malagasy Endemic Plant</a>, CHEMICAL & PHARMACEUTICAL BULLETIN. 2002 Jan | journal-article. doi: 10.1248/cpb.50.1122.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0036814921&partnerID=MN8TOARS' target='_blank' class='bux-link'>A new secoiridoid glucoside from a malagasy medicinal plant, Cassinopsis chapieleri</a>, Natural Medicines. 2002 Jan | journal-article. .

<a href='' target='_blank' class='bux-link'>Cussosaponins A—E, Triterpene Saponins from the Leaves of Cussonia racemosa, a Malagasy Endemic Plant</a>, CHEMICAL & PHARMACEUTICAL BULLETIN. 2002 Jan | journal-article. doi: 10.1248/cpb.50.1290.

<a href='' target='_blank' class='bux-link'>Ent-kaurane Diterpenoid Glycosides from the Leaves of Cussonia racemosa, a Malagasy Endemic Plant</a>, CHEMICAL & PHARMACEUTICAL BULLETIN. 2002 Jan | journal-article. doi: 10.1248/cpb.50.268.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0036814717&partnerID=MN8TOARS' target='_blank' class='bux-link'>Iridoid glucosides from a malagasy medicinal plant, Ophiocolea floribunda</a>, Natural Medicines. 2002 Jan | journal-article. .

<a href='' target='_blank' class='bux-link'>Composition and Antimicrobial Activity of Leaf Oils of Vepris leandriana H. Perr.</a>, Journal of Essential Oil Research. 2001 Nov | journal-article. doi: 10.1080/10412905.2001.9699731.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0034820676&partnerID=MN8TOARS' target='_blank' class='bux-link'>New iridoid and phenethyl glycosides from Malagasy medicinal plant, Phyllarthron madagascariense</a>, Natural Medicines. 2001 Jan | journal-article. .

Blake R. Peterson

Chair of the Division of Medicinal Chemistry & Pharmacognosy

Professor

Medicinal Chemistry and Pharmacognosy

College Administration

Research Areas

Cancer,

Medicinal Chemistry & Pharmacognosy,

Chemical Biology,

Chemical Synthesis

606 Riffe Building

peterson.1119@osu.edu

(614) 247-7729

Professional Website

Dr. Peterson’s research group works to design, synthesize, and discover small molecules that affect the proliferation of cancer cells and associated immune cells that support malignancy. To identify these compounds, the Peterson laboratory synthesizes fluorescent molecular probes as tools for drug discovery. These probes are used to create target-based or phenotypic drug discovery assays to identify anticancer agents with novel mechanisms of action. To optimize and evaluate these compounds, they use synthetic organic chemistry, medicinal chemistry, and chemical biology approaches. In conjunction with high throughput screening by confocal microscopy, flow cytometry, and other related techniques, his laboratory identifies chemical probes of biological systems, uncovers mechanisms of biologically active agents, and discovers hit and lead compounds for the development of therapeutics.

Dr. Peterson’s educational background includes a BS in Chemistry from the University of Nevada Reno, a PhD in Chemistry from the University of California, Los Angeles, and postdoctoral training at Harvard University in the Department of Chemistry and Chemical Biology as a Damon Runyon / Walter Winchell Cancer Research fellow. His first independent faculty position was at Penn State University, where he was an assistant and tenured associate professor of Chemistry. During this time, he co-founded Indigo Biosciences Inc., a leading provider of nuclear receptor and in vitro toxicology solutions that accelerate scientific decision-making. He later moved to the University of Kansas as a Regents Distinguished Professor of Medicinal Chemistry. In 2019, he joined the faculty of The Ohio State University College of Pharmacy as Professor and Chair of the Division of Medicinal Chemistry and Pharmacognosy. He additionally holds appointments at the Ohio State University Comprehensive Cancer Center as Co-Leader of the Translational Therapeutics Program and Co-Director of the Medicinal Chemistry Shared Resource.

B.S. Chemistry, University of Nevada, Reno, 1990

Ph.D. Chemistry, University of California, Los Angeles, 1994

Damon Runyon-Walter Winchell Cancer Research Foundation Postdoctoral Fellow, Harvard University 1995-1998

Named the John W. Wolfe Chair in Cancer Research, 2020

Elected Fellow of the American Association for the Advancement of Science (AAAS), 2013

Regents Distinguished Professor of Medicinal Chemistry, The University of Kansas, 2008-2019

Leading Light Research Award, 2012

Named an Eminent Scholar by the Kansas Bioscience Authority, 2008

Elected Co-Chair of the 2007 Gordon Conference on Bioorganic Chemistry

Camille Dreyfus Teacher Scholar, 2004

American Cancer Society Research Scholar, 2003

<a href='https://doi.org/10.1021/acsmedchemlett.4c00085' target='_blank' class='bux-link'>Synthesis of Monofluorinated 7-Hydroxycoumarin-3-Carboxamides as Cell-Permeable Fluorescent Molecular Probes</a>, ACS Medicinal Chemistry Letters. 2024 Apr | journal-article. doi: 10.1021/acsmedchemlett.4c00085.

<a href='https://doi.org/10.1021/jacs.3c07488' target='_blank' class='bux-link'>Quantification of Binding of Small Molecules to Native Proteins Overexpressed in Living Cells</a>, Journal of the American Chemical Society. 2024 Jan | journal-article. doi: 10.1021/jacs.3c07488.

<a href='http://dx.doi.org/10.1038/s41375-023-02006-8' target='_blank' class='bux-link'>Exploiting the fibroblast growth factor receptor-1 vulnerability to therapeutically restrict the MYC-EZH2-CDKN1C axis-driven proliferation in Mantle cell lymphoma</a>, Leukemia. 2023 Oct | journal-article. doi: 10.1038/s41375-023-02006-8.

<a href='https://doi.org/10.1021/acsptsci.3c00014' target='_blank' class='bux-link'>Fluorescent Detection of Peroxynitrite Produced by Myeloid-Derived Suppressor Cells in Cancer and Inhibition by Dasatinib</a>, ACS Pharmacology & Translational Science. 2023 May | journal-article. doi: 10.1021/acsptsci.3c00014.

<a href='https://doi.org/10.1002/chem.202300315' target='_blank' class='bux-link'>Photoluminescent Properties and Mechanism of Novel Cyanine‐Borondifluoride Curcuminoid Hybrids as Red‐to‐Near Infrared and Endoplasmic Reticulum‐Targeting Dyes</a>, Chemistry – A European Journal. 2023 Apr | journal-article. doi: 10.1002/chem.202300315.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85166303613&partnerID=MN8TOARS' target='_blank' class='bux-link'>BTK inhibition potentiates anti-PD-L1 treatment in murine melanoma: potential role for MDSC modulation in immunotherapy</a>, Cancer Immunology, Immunotherapy. 2023 Jan | journal-article. doi: 10.1007/s00262-023-03497-1.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85172813705&partnerID=MN8TOARS' target='_blank' class='bux-link'>Successful Orthotopic Liver Transplantation in Mice Utilizing Microcomputed Tomography Angiography</a>, Journal of Visualized Experiments. 2023 Jan | journal-article. doi: 10.3791/65537.

<a href='https://doi.org/10.1021/acsbiomedchemau.2c00031' target='_blank' class='bux-link'>Quantification of Engagement of Microtubules by Small Molecules in Living Cells by Flow Cytometry</a>, ACS Bio & Med Chem Au. 2022 Oct | journal-article. doi: 10.1021/acsbiomedchemau.2c00031.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85129621384&partnerID=MN8TOARS' target='_blank' class='bux-link'>Pacific Blue-Taxoids as Fluorescent Molecular Probes of Microtubules</a>, Methods in Molecular Biology. 2022 Jan | book. doi: 10.1007/978-1-0716-1983-4_28.

<a href='https://doi.org/10.1039/D1MD00395J' target='_blank' class='bux-link'>Synthesis of a fluorinated pyronin that enables blue light to rapidly depolarize mitochondria</a>, RSC Medicinal Chemistry. 2022 Jan | journal-article. doi: 10.1039/D1MD00395J.

<a href='https://www.mdpi.com/2227-9059/9/5/477' target='_blank' class='bux-link'>Carnosine Protects Macrophages against the Toxicity of Aβ1-42 Oligomers by Decreasing Oxidative Stress</a>, Biomedicines. 2021 Apr | journal-article. doi: 10.3390/biomedicines9050477.

<a href='https://doi.org/10.1371/journal.ppat.1008134' target='_blank' class='bux-link'>The C. elegans CHP1 homolog, pbo-1, functions in innate immunity by regulating the pH of the intestinal lumen</a>, PLOS Pathogens. 2020 Jan | journal-article. doi: 10.1371/journal.ppat.1008134.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85084740254&partnerID=MN8TOARS' target='_blank' class='bux-link'>Fluorescent detection of peroxynitrite during antibody-dependent cellular phagocytosis</a>, Methods in Enzymology. 2020 Jan | book. doi: 10.1016/bs.mie.2020.04.001.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85078658353&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthetic Rhamnose Glycopolymer Cell-Surface Receptor for Endogenous Antibody Recruitment</a>, Biomacromolecules. 2020 Jan | journal-article. doi: 10.1021/acs.biomac.9b01483.

<a href='https://doi.org/10.1039/C9CC09598E' target='_blank' class='bux-link'>Visible photorelease of liquid biopsy markers following microfluidic affinity-enrichment</a>, Chemical Communications. 2020 Jan | journal-article. doi: 10.1039/C9CC09598E.

<a href='https://doi.org/10.1021/acsomega.9b01585' target='_blank' class='bux-link'>Antibody–Drug Conjugate that Exhibits Synergistic Cytotoxicity with an Endosome–Disruptive Peptide</a>, ACS Omega. 2019 Jul | journal-article. doi: 10.1021/acsomega.9b01585.

<a href='https://doi.org/10.1021/jacs.9b00394' target='_blank' class='bux-link'>Small Molecule Inhibitors of the BfrB–Bfd Interaction Decrease Pseudomonas aeruginosa Fitness and Potentiate Fluoroquinolone Activity</a>, Journal of the American Chemical Society. 2019 May | journal-article. doi: 10.1021/jacs.9b00394.

<a href='https://doi.org/10.1021/acschembio.8b00535' target='_blank' class='bux-link'>Targeting Fluorescent Sensors to Endoplasmic Reticulum Membranes Enables Detection of Peroxynitrite During Cellular Phagocytosis</a>, ACS Chemical Biology. 2018 Sep | journal-article. doi: 10.1021/acschembio.8b00535.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85049195920&partnerID=MN8TOARS' target='_blank' class='bux-link'>Malleilactone is a Burkholderia pseudomallei virulence factor regulated by antibiotics and quorum sensing</a>, Journal of Bacteriology. 2018 Jan | journal-article. doi: 10.1128/JB.00008-18.

<a href='https://doi.org/10.1002/anie.201703298' target='_blank' class='bux-link'>Synthesis of a Fluorescent Analogue of Paclitaxel That Selectively Binds Microtubules and Sensitively Detects Efflux by P‐Glycoprotein</a>, Angewandte Chemie International Edition. 2017 Jun | journal-article. doi: 10.1002/anie.201703298.

<a href='https://doi.org/10.1021/acsomega.6b00356' target='_blank' class='bux-link'>Quantification of Small Molecule–Protein Interactions using FRET between Tryptophan and the Pacific Blue Fluorophore</a>, ACS Omega. 2016 Dec | journal-article. doi: 10.1021/acsomega.6b00356.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84967166946&partnerID=MN8TOARS' target='_blank' class='bux-link'>Hydrophobic resorufamine derivatives: Potent and selective red fluorescent probes of the endoplasmic reticulum of mammalian cells</a>, Dyes and Pigments. 2016 Jan | journal-article. doi: 10.1016/j.dyepig.2016.05.007.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84923321861&partnerID=MN8TOARS' target='_blank' class='bux-link'>Anticancer/antiviral agent Akt inhibitor-iv massively accumulates in mitochondria and potently disrupts cellular bioenergetics</a>, ACS Chemical Biology. 2015 Jan | journal-article. doi: 10.1021/cb500856c.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84941896950&partnerID=MN8TOARS' target='_blank' class='bux-link'>Fluorescent mimics of cholesterol that rapidly bind surfaces of living mammalian cells</a>, Chemical Communications. 2015 Jan | journal-article. doi: 10.1039/c5cc06325f.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84938416839&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of Fluorophores that Target Small Molecules to the Endoplasmic Reticulum of Living Mammalian Cells</a>, Angewandte Chemie - International Edition. 2015 Jan | journal-article. doi: 10.1002/anie.201504156.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84898003389&partnerID=MN8TOARS' target='_blank' class='bux-link'>Detection of protein-protein interactions by proximity-driven S <inf>N</inf>Ar reactions of lysine-linked fluorophores</a>, Journal of the American Chemical Society. 2014 Jan | journal-article. doi: 10.1021/ja501253b.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84893873866&partnerID=MN8TOARS' target='_blank' class='bux-link'>Efficient and scalable synthesis of 4-carboxy-pennsylvania green methyl ester: A hydrophobic building block for fluorescent molecular probes</a>, Synthesis (Germany). 2014 Jan | journal-article. doi: 10.1055/s-0033-1338535.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84880901358&partnerID=MN8TOARS' target='_blank' class='bux-link'>Decreased APOE-containing HDL subfractions and cholesterol efflux capacity of serum in mice lacking Pcsk9</a>, Lipids in Health and Disease. 2013 Jan | journal-article. doi: 10.1186/1476-511X-12-112.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84875168987&partnerID=MN8TOARS' target='_blank' class='bux-link'>Novel acid-activated fluorophores reveal a dynamic wave of protons in the intestine of caenorhabditis elegans</a>, ACS Chemical Biology. 2013 Jan | journal-article. doi: 10.1021/cb300396j.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84871042909&partnerID=MN8TOARS' target='_blank' class='bux-link'>Hydrophobic analogues of rhodamine B and rhodamine 101: Potent fluorescent probes of mitochondria in living C. elegans</a>, Beilstein Journal of Organic Chemistry. 2012 Jan | journal-article. doi: 10.3762/bjoc.8.243.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84860126819&partnerID=MN8TOARS' target='_blank' class='bux-link'>Identification of a small molecule yeast TORC1 inhibitor with a multiplex screen based on flow cytometry</a>, ACS Chemical Biology. 2012 Jan | journal-article. doi: 10.1021/cb200452r.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84855688694&partnerID=MN8TOARS' target='_blank' class='bux-link'>Interaction of 3β-amino-5-cholestene with phospholipids in binary and ternary bilayer membranes</a>, Langmuir. 2012 Jan | journal-article. doi: 10.1021/la203589u.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84870774679&partnerID=MN8TOARS' target='_blank' class='bux-link'>Sensitivity of Mitochondrial Transcription and Resistance of RNA Polymerase II Dependent Nuclear Transcription to Antiviral Ribonucleosides</a>, PLoS Pathogens. 2012 Jan | journal-article. doi: 10.1371/journal.ppat.1003030.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84855557822&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of fluorinated benzophenones, xanthones, acridones, and thioxanthones by iterative nucleophilic aromatic substitution</a>, Journal of Organic Chemistry. 2012 Jan | journal-article. doi: 10.1021/jo202062f.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84861229000&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthetic cell surface receptors for delivery of therapeutics and probes</a>, Advanced Drug Delivery Reviews. 2012 Jan | journal-article. doi: 10.1016/j.addr.2012.02.007.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84859756203&partnerID=MN8TOARS' target='_blank' class='bux-link'>Targeting of histone acetyltransferase p300 by cyclopentenone prostaglandin Δ 12-PGJ 2 through covalent binding to Cys 1438</a>, Chemical Research in Toxicology. 2012 Jan | journal-article. doi: 10.1021/tx200383c.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-79953784003&partnerID=MN8TOARS' target='_blank' class='bux-link'>Development of a cell-based, high-throughput screening assay for cholesterol efflux using a fluorescent mimic of cholesterol</a>, Assay and Drug Development Technologies. 2011 Jan | journal-article. doi: 10.1089/adt.2010.0288.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-80052185689&partnerID=MN8TOARS' target='_blank' class='bux-link'>Human neutrophil peptides mediate endothelial-monocyte interaction, foam cell formation, and platelet activation</a>, Arteriosclerosis, Thrombosis, and Vascular Biology. 2011 Jan | journal-article. doi: 10.1161/ATVBAHA.111.227116.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-79958761265&partnerID=MN8TOARS' target='_blank' class='bux-link'>Structural requirements for the inhibition of calcium mobilization and mast cell activation by the pyrazole derivative BTP2</a>, International Journal of Biochemistry and Cell Biology. 2011 Jan | journal-article. doi: 10.1016/j.biocel.2011.04.016.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-79952259137&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and biological evaluation of analogues of AKT (protein kinase B) inhibitor-IV</a>, Journal of Medicinal Chemistry. 2011 Jan | journal-article. doi: 10.1021/jm100912b.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-73749083079&partnerID=MN8TOARS' target='_blank' class='bux-link'>Chemico-genetic identification of drebrin as a regulator of calcium responses</a>, International Journal of Biochemistry and Cell Biology. 2010 Jan | journal-article. doi: 10.1016/j.biocel.2009.11.019.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-78649494373&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of a 6-methyl-7-deaza analogue of adenosine that potently inhibits replication of polio and dengue viruses</a>, Journal of Medicinal Chemistry. 2010 Jan | journal-article. doi: 10.1021/jm100593s.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-60849111993&partnerID=MN8TOARS' target='_blank' class='bux-link'>Practical synthesis of 3β-amino-5-cholestene and related 3β-halides involving i-steroid and retro-i-steroid rearrangements</a>, Organic Letters. 2009 Jan | journal-article. doi: 10.1021/ol802343z.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-41249093707&partnerID=MN8TOARS' target='_blank' class='bux-link'>Antibacterial and hemolytic activities of pyridinium polymers as a function of the spatial relationship between the positive charge and the pendant alkyl tail</a>, Angewandte Chemie - International Edition. 2008 Jan | journal-article. doi: 10.1002/anie.200702287.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-40549143689&partnerID=MN8TOARS' target='_blank' class='bux-link'>Lethal mutagenesis of picornaviruses with N-6-modified purine nucleoside analogues</a>, Antimicrobial Agents and Chemotherapy. 2008 Jan | journal-article. doi: 10.1128/AAC.01056-07.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-47949094109&partnerID=MN8TOARS' target='_blank' class='bux-link'>Multifunctional silane polymers for persistent surface derivatization and their antimicrobial properties</a>, Langmuir. 2008 Jan | journal-article. doi: 10.1021/la800858z.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-48849091987&partnerID=MN8TOARS' target='_blank' class='bux-link'>One-pot synthesis of nucleoside 5 -triphosphates from nucleoside 5 -H-phosphonates</a>, Organic Letters. 2008 Jan | journal-article. doi: 10.1021/ol8003029.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-48749090741&partnerID=MN8TOARS' target='_blank' class='bux-link'>Selective disruption of early/recycling endosomes: Release of disulfide-linked cargo mediated by a N-alkyl-3β-cholesterylamine-capped peptide</a>, Journal of the American Chemical Society. 2008 Jan | journal-article. doi: 10.1021/ja803380a.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-43149087336&partnerID=MN8TOARS' target='_blank' class='bux-link'>Structural insights into mechanisms of catalysis and inhibition in Norwalk virus polymerase</a>, Journal of Biological Chemistry. 2008 Jan | journal-article. doi: 10.1074/jbc.M709563200.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-34848924589&partnerID=MN8TOARS' target='_blank' class='bux-link'>A concise synthesis of the pennsylvania green fluorophore and labeling of intracellular targets with O 6-benzylguanine derivatives</a>, Organic Letters. 2007 Jan | journal-article. doi: 10.1021/ol7015093.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33846212777&partnerID=MN8TOARS' target='_blank' class='bux-link'>Endocytic delivery of vancomycin mediated by a synthetic cell surface receptor: Rescue of bacterially infected mammalian cells and tissue targeting in vivo</a>, Journal of the American Chemical Society. 2007 Jan | journal-article. doi: 10.1021/ja067674f.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-35148825918&partnerID=MN8TOARS' target='_blank' class='bux-link'>Lethal mutagenesis of poliovirus mediated by a mutagenic pyrimidine analogue</a>, Journal of Virology. 2007 Jan | journal-article. doi: 10.1128/JVI.01028-07.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-36549042007&partnerID=MN8TOARS' target='_blank' class='bux-link'>Model systems. Mimics and probes of biological systems</a>, Current Opinion in Chemical Biology. 2007 Jan | journal-article. doi: 10.1016/j.cbpa.2007.10.010.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-34548124606&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of a universal 5-nitroindole ribonucleotide and incorporation into RNA by a viral RNA-dependent RNA polymerase</a>, ChemBioChem. 2007 Jan | journal-article. doi: 10.1002/cbic.200700160.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33947241783&partnerID=MN8TOARS' target='_blank' class='bux-link'>The oxidative stress mediator 4-hydroxynonenal is an intracellular agonist of the nuclear receptor peroxisome proliferator-activated receptor-β/δ (PPARβ/δ)</a>, Free Radical Biology and Medicine. 2007 Jan | journal-article. doi: 10.1016/j.freeradbiomed.2007.01.003.

<a href='http://dx.doi.org/10.1021/ja056126j' target='_blank' class='bux-link'>Synthesis of an Artificial Cell Surface Receptor that Enables Oligohistidine Affinity Tags to Function as Metal-Dependent Cell-Penetrating Peptides</a>, Journal of the American Chemical Society. 2006 Jan | journal-article. doi: 10.1021/ja056126j.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33748371420&partnerID=MN8TOARS' target='_blank' class='bux-link'>A synthetic mimic of human Fc receptors: Defined chemical modification of cell surfaces enables efficient endocytic uptake of human immunoglobulin-G</a>, Journal of the American Chemical Society. 2006 Jan | journal-article. doi: 10.1021/ja062377w.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33746602684&partnerID=MN8TOARS' target='_blank' class='bux-link'>Silver bromide nanoparticle/polymer composites: Dual action tunable antimicrobial materials</a>, Journal of the American Chemical Society. 2006 Jan | journal-article. doi: 10.1021/ja061442z.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-38549153858&partnerID=MN8TOARS' target='_blank' class='bux-link'>Small-molecule triggers of tadpole metamorphosis.</a>, ACS chemical biology. 2006 Jan | journal-article. doi: 10.1021/cb600398a.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33750111990&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and antiviral activity of 5-substituted cytidine analogues: Identification of a potent inhibitor of viral RNA-dependent RNA polymerases</a>, Journal of Medicinal Chemistry. 2006 Jan | journal-article. doi: 10.1021/jm060872x.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33644759177&partnerID=MN8TOARS' target='_blank' class='bux-link'>The Pennsylvania Green fluorophore: A hybrid of Oregon Green and Tokyo Green for the construction of hydrophobic and pH-insensitive molecular probes</a>, Organic Letters. 2006 Jan | journal-article. doi: 10.1021/ol052655g.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-23844514425&partnerID=MN8TOARS' target='_blank' class='bux-link'>Calcium flux in neuroblastoma cells is a coupling mechanism between non-genomic and genomic modes of estrogens</a>, Neuroendocrinology. 2005 Jan | journal-article. doi: 10.1159/000087000.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-23744481464&partnerID=MN8TOARS' target='_blank' class='bux-link'>Fluorescence-based cloning of a protein tyrosine kinase with a yeast tribrid system</a>, ChemBioChem. 2005 Jan | journal-article. doi: 10.1002/cbic.200500047.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-27744563015&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthetic mimics of mammalian cell surface receptors: Prosthetic molecules that augment living cells</a>, Organic and Biomolecular Chemistry. 2005 Jan | journal-article. doi: 10.1039/b509866a.

<a href='http://dx.doi.org/10.1002/anie.200460489' target='_blank' class='bux-link'>An Amphotericin B–Fluorescein Conjugate as a Powerful Probe for Biochemical Studies of the Membrane</a>, Angewandte Chemie International Edition. 2004 Oct | journal-article. doi: 10.1002/anie.200460489.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-4744346088&partnerID=MN8TOARS' target='_blank' class='bux-link'>11β-alkyl-Δ9-19-nortestosterone derivatives: High-affinity ligands and potent partial agonists of the androgen receptor</a>, Journal of Medicinal Chemistry. 2004 Jan | journal-article. doi: 10.1021/jm0342515.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-2442570963&partnerID=MN8TOARS' target='_blank' class='bux-link'>Facile synthesis of CIDs: Biotinylated estrone oximes efficiently heterodimerize estrogen receptor and streptavidin proteins in yeast three hybrid systems</a>, Organic Letters. 2004 Jan | journal-article. doi: 10.1021/ol0497537.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-1642301066&partnerID=MN8TOARS' target='_blank' class='bux-link'>Molecule-Specific Imaging with Mass Spectrometry and a Buckminsterfullerene Probe: Application to Characterizing Solid-Phase Synthesized Combinatorial Libraries</a>, Journal of the American Chemical Society. 2004 Jan | journal-article. doi: 10.1021/ja036549q.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-11444262104&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthetic mimics of small mammalian cell surface receptors</a>, Journal of the American Chemical Society. 2004 Jan | journal-article. doi: 10.1021/ja046663o.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0037415010&partnerID=MN8TOARS' target='_blank' class='bux-link'>Analysis of protein tyrosine kinase inhibitors in recombinant yeast lacking the ERG6 gene</a>, ChemBioChem. 2003 Jan | journal-article. doi: 10.1002/cbic.200390001.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0346968185&partnerID=MN8TOARS' target='_blank' class='bux-link'>Control of Gene Expression with Small Molecules: Biotin-Mediated Acylation of Targeted Lysine Residues in Recombinant Yeast</a>, Chemistry and Biology. 2003 Jan | journal-article. doi: 10.1016/j.chembiol.2003.11.007.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0141572110&partnerID=MN8TOARS' target='_blank' class='bux-link'>Fluorescent cellular sensors of steroid receptor ligands</a>, ChemBioChem. 2003 Jan | journal-article. doi: 10.1002/cbic.200300606.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0037257708&partnerID=MN8TOARS' target='_blank' class='bux-link'>Non-natural cell surface receptors: Synthetic peptides capped with N-cholesterylglycine efficiently deliver proteins into mammalian cells</a>, Bioconjugate Chemistry. 2003 Jan | journal-article. doi: 10.1021/bc025601p.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0042334826&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of a high-affinity Fluorescent PPARγ ligand for high-throughput fluorescence polarization assays</a>, Bioorganic and Medicinal Chemistry. 2003 Jan | journal-article. doi: 10.1016/S0968-0896(03)00494-2.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0037414262&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of a β-estradiol-biotin chimera that potently heterodimerizes estrogen receptor and streptavidin proteins in a yeast three-hybrid system</a>, Journal of the American Chemical Society. 2003 Jan | journal-article. doi: 10.1021/ja0293305.

<a href='http://dx.doi.org/10.1002/psc.376' target='_blank' class='bux-link'>A colorimetric enzyme‐linked on‐bead assay for identification of synthetic substrates of protein tyrosine kinases</a>, Journal of Peptide Science. 2002 May | journal-article. doi: 10.1002/psc.376.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0036750823&partnerID=MN8TOARS' target='_blank' class='bux-link'>A fluorescence-based high performance liquid chromatographic method for the characterization of palmitoyl acyl transferase activity</a>, Analytical Biochemistry. 2002 Jan | journal-article. doi: 10.1016/S0003-2697(02)00212-9.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0036918297&partnerID=MN8TOARS' target='_blank' class='bux-link'>Augmenting vitamin D to combat genetic disease</a>, Chemistry and Biology. 2002 Jan | journal-article. doi: 10.1016/S1074-5521(02)00287-9.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0037024177&partnerID=MN8TOARS' target='_blank' class='bux-link'>Efficient delivery of streptavidin to mammalian cells: Clathrin-mediated endocytosis regulated by a synthetic ligand</a>, Journal of the American Chemical Society. 2002 Jan | journal-article. doi: 10.1021/ja0258733.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0036589848&partnerID=MN8TOARS' target='_blank' class='bux-link'>Rapid detection of protein tyrosine kinase activity in recombinant yeast expressing a universal substrate</a>, Journal of Proteome Research. 2002 Jan | journal-article. doi: 10.1021/pr0255093.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0037139566&partnerID=MN8TOARS' target='_blank' class='bux-link'>Sensitive and rapid analysis of protein palmitoylation with a synthetic cell-permeable mimic of Src oncoproteins</a>, Journal of the American Chemical Society. 2002 Jan | journal-article. doi: 10.1021/ja017671x.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0037162434&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and antiviral evaluation of a mutagenic and non-hydrogen bonding ribonucleoside analogue: 1-β-D-ribofuranosyl-3-nitropyrrole</a>, Biochemistry. 2002 Jan | journal-article. doi: 10.1021/bi026120w.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0037034312&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of chimeric 7α-substituted estradiol derivatives linked to cholesterol and cholesterylamine</a>, Organic Letters. 2002 Jan | journal-article. doi: 10.1021/ol0171261.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0035915381&partnerID=MN8TOARS' target='_blank' class='bux-link'>A synthetic membrane-anchored antigen efficiently promotes uptake of antifluorescein antibodies and associated protein A by mammalian cells</a>, Journal of the American Chemical Society. 2001 Jan | journal-article. doi: 10.1021/ja017087o.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0003144837&partnerID=MN8TOARS' target='_blank' class='bux-link'>Macrotricyclic Steroid Receptors by Pd°-Catalyzed Cross-Coupling Reactions: Dissolution of Cholesterol in Aqueous Solution and Investigations of the Principles Governing Selective Molecular Recognition of Steroidal Substrates</a>, Helvetica Chimica Acta. 1998 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0032564466&partnerID=MN8TOARS' target='_blank' class='bux-link'>The orientation of the AP-1 heterodimer on DNA strongly affects transcriptional potency</a>, Proceedings of the National Academy of Sciences of the United States of America. 1998 Jan | journal-article. doi: 10.1073/pnas.95.24.14076.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0030974118&partnerID=MN8TOARS' target='_blank' class='bux-link'>Dual role of the nuclear factor of activated T cells insert region in DNA recognition and cooperative contacts to activator protein</a>, Proceedings of the National Academy of Sciences of the United States of America. 1997 Jan | journal-article. doi: 10.1073/pnas.94.10.4919.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-12644271902&partnerID=MN8TOARS' target='_blank' class='bux-link'>A critical arginine residue mediates cooperativity in the contact interface between transcription factors NFAT and AP-1</a>, Proceedings of the National Academy of Sciences of the United States of America. 1996 Jan | journal-article. doi: 10.1073/pnas.93.24.13671.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0029257720&partnerID=MN8TOARS' target='_blank' class='bux-link'>Cavity depth and width effects on cyclophane-steroid recognition: molecular complexation of cholesterol and progesterone in aqueous solution</a>, Chemistry and Biology. 1995 Jan | journal-article. doi: 10.1016/1074-5521(95)90068-3.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0028939372&partnerID=MN8TOARS' target='_blank' class='bux-link'>Steroid complexation by cyclophane receptors in aqueous solution: Substrate selectivity, enthalpic driving force for cavity inclusion, and enthalpy-entropy compensation</a>, Tetrahedron. 1995 Jan | journal-article. doi: 10.1016/0040-4020(94)00905-A.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0028280962&partnerID=MN8TOARS' target='_blank' class='bux-link'>Bilirubin Conformational Analysis and Circular Dichroism</a>, Journal of the American Chemical Society. 1994 Jan | journal-article. doi: 10.1021/ja00080a006.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33748828605&partnerID=MN8TOARS' target='_blank' class='bux-link'>Dissolution of Cholesterol in Water by a Synthetic Receptor</a>, Angewandte Chemie International Edition in English. 1994 Jan | journal-article. doi: 10.1002/anie.199416251.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0025795823&partnerID=MN8TOARS' target='_blank' class='bux-link'>Conformational analysis and circular dichroism of bilirubin, the yellow pigment of jaundice</a>, Proceedings of SPIE - The International Society for Optical Engineering. 1991 Jan | conference-paper. .

Mark Mitton-Fry

Associate Professor

Medicinal Chemistry and Pharmacognosy

Research Areas

Infectious Diseases,

Medicinal Chemistry & Pharmacognosy

Parks Hall

mitton-fry.1@osu.edu

(614) 292-1903

Professional Website

Dr. Mitton-Fry’s research team is dedicated to inventing cures for multidrug-resistant bacterial infections. The lab uses the tools of synthetic medicinal chemistry to design and prepare innovative new molecules, and we collaborate broadly to evaluate their biological, pharmaceutical, and toxicological properties. Dr. Mitton-Fry also enjoys teaching students at all levels about antibacterial therapies.

2002, PhD, University of Colorado Boulder

1996, BA, Carleton College

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85167914159&partnerID=MN8TOARS' target='_blank' class='bux-link'>Actions of a Novel Bacterial Topoisomerase Inhibitor against Neisseria gonorrhoeae Gyrase and Topoisomerase IV: Enhancement of Double-Stranded DNA Breaks</a>, International Journal of Molecular Sciences. 2023 Jan | journal-article. doi: 10.3390/ijms241512107.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85166353241&partnerID=MN8TOARS' target='_blank' class='bux-link'>Antibacterial activity of novel bacterial topoisomerase inhibitors against key veterinary pathogens</a>, Veterinary Microbiology. 2023 Jan | journal-article. doi: 10.1016/j.vetmic.2023.109840.

<a href='' target='_blank' class='bux-link'>Serendipitous Discovery of a Competitive Inhibitor of FraB, a Salmonella Deglycase and Drug Target</a>, Pathogens. 2022 Sep | journal-article. doi: 10.3390/pathogens11101102.

<a href='' target='_blank' class='bux-link'>Aryl Methyl Ketones: Versatile Synthons in the Synthesis of Heterocyclic Compounds</a>, SynOpen. 2022 Jun | journal-article. doi: 10.1055/a-1826-2852.

<a href='' target='_blank' class='bux-link'>1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum</a>, ACS Medicinal Chemistry Letters. 2022 May | journal-article. doi: 10.1021/acsmedchemlett.2c00111.

<a href='' target='_blank' class='bux-link'>Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors Exhibit Bactericidal Activity against Planktonic and Biofilm Staphylococcus aureus In Vitro</a>, Microbiology Spectrum. 2022 Jan | journal-article. doi: 10.1128/spectrum.02056-22.

<a href='https://doi.org/10.1021/acs.jmedchem.1c01250' target='_blank' class='bux-link'>Optimization of TopoIV Potency, ADMET Properties, and hERG Inhibition of 5-Amino-1,3-dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Identification of a Lead with In Vivo Efficacy against MRSA.</a>, Journal of medicinal chemistry. 2021 Oct | journal-article. doi: 10.1021/acs.jmedchem.1c01250.

<a href='https://doi.org/10.1016/j.ejmech.2020.112324' target='_blank' class='bux-link'>Novel bacterial topoisomerase inhibitors derived from isomannide.</a>, European journal of medicinal chemistry. 2020 Apr | journal-article. doi: 10.1016/j.ejmech.2020.112324.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85096045755&partnerID=MN8TOARS' target='_blank' class='bux-link'>Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-Positive Staphylococcus aureus</a>, ACS Medicinal Chemistry Letters. 2020 Jan | journal-article. doi: 10.1021/acsmedchemlett.0c00428.

<a href='http://dx.doi.org/10.1021/acsinfecdis.8b00375' target='_blank' class='bux-link'>1,3-Dioxane-Linked Bacterial Topoisomerase Inhibitors with Enhanced Antibacterial Activity and Reduced hERG Inhibition</a>, . 2019 May | journal-article. doi: 10.1021/acsinfecdis.8b00375.

<a href='' target='_blank' class='bux-link'>Process Development for the Synthesis of Monocyclic β-Lactam Core 17</a>, Organic Process Research & Development. 2018 Jan | journal-article. doi: 10.1021/acs.oprd.7b00359.

<a href='' target='_blank' class='bux-link'>Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases</a>, Journal of Medicinal Chemistry. 2018 Jan | journal-article. doi: 10.1021/acs.jmedchem.7b01598.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85047875979&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety</a>, Bioorganic and Medicinal Chemistry Letters. 2018 Jan | journal-article. doi: 10.1016/j.bmcl.2018.06.003.

<a href='' target='_blank' class='bux-link'>Novel Bacterial Type II Topoisomerase Inhibitors</a>, 2017 Medicinal Chemistry Reviews. 2017 Nov | other. doi: 10.29200/acsmedchemrev-v52.ch15.

<a href='' target='_blank' class='bux-link'>Novel 3-fluoro-6-methoxyquinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV</a>, Bioorganic & Medicinal Chemistry Letters. 2017 Aug | journal-article. doi: 10.1016/j.bmcl.2017.06.009.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84939144713&partnerID=MN8TOARS' target='_blank' class='bux-link'>Corrigendum to "Novel monobactams utilizing a siderophore uptake mechanism for the treatment of Gram-negative infections" [Bioorg. Med. Chem. Lett. 22/18 (2012) 5989-5994]</a>, Bioorganic and Medicinal Chemistry Letters. 2015 Jan | journal-article. doi: 10.1016/j.bmcl.2015.07.024.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84903820508&partnerID=MN8TOARS' target='_blank' class='bux-link'>Oclacitinib (APOQUEL®) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy</a>, Journal of Veterinary Pharmacology and Therapeutics. 2014 Jan | journal-article. doi: 10.1111/jvp.12101.

<a href='' target='_blank' class='bux-link'>Pyridone-Conjugated Monobactam Antibiotics with Gram-Negative Activity</a>, Journal of Medicinal Chemistry. 2013 Jul | journal-article. doi: 10.1021/jm400560z.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84876673641&partnerID=MN8TOARS' target='_blank' class='bux-link'>Novel quinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV</a>, Bioorganic and Medicinal Chemistry Letters. 2013 Jan | journal-article. doi: 10.1016/j.bmcl.2013.03.047.

<a href='' target='_blank' class='bux-link'>Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents</a>, Bioorganic & Medicinal Chemistry Letters. 2012 Nov | journal-article. doi: 10.1016/j.bmcl.2012.09.058.

<a href='' target='_blank' class='bux-link'>Total synthesis of (±)-monomorine</a>, Tetrahedron Letters. 2012 Oct | journal-article. doi: 10.1016/j.tetlet.2012.08.041.

<a href='' target='_blank' class='bux-link'>Rapid Evaluation in Whole Blood Culture of Regimens for XDR-TB Containing PNU-100480 (Sutezolid), TMC207, PA-824, SQ109, and Pyrazinamide</a>, PLoS ONE. 2012 Jan | journal-article. doi: 10.1371/journal.pone.0030479.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84865519152&partnerID=MN8TOARS' target='_blank' class='bux-link'>Novel monobactams utilizing a siderophore uptake mechanism for the treatment of gram-negative infections</a>, Bioorganic and Medicinal Chemistry Letters. 2012 Jan | journal-article. doi: 10.1016/j.bmcl.2012.07.005.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84863119192&partnerID=MN8TOARS' target='_blank' class='bux-link'>Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious Gram-negative infections</a>, Journal of Medicinal Chemistry. 2012 Jan | journal-article. doi: 10.1021/jm2014875.

<a href='' target='_blank' class='bux-link'>Total Synthesis of Dermostatin A</a>, The Journal of Organic Chemistry. 2011 Oct | journal-article. doi: 10.1021/jo2012658.

<a href='' target='_blank' class='bux-link'>Preparation, Gram-Negative Antibacterial Activity, and Hydrolytic Stability of Novel Siderophore-Conjugated Monocarbam Diols</a>, ACS Medicinal Chemistry Letters. 2011 May | journal-article. doi: 10.1021/ml200012f.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-78751693374&partnerID=MN8TOARS' target='_blank' class='bux-link'>Biomarker-assisted dose selection for safety and efficacy in early development of PNU-100480 for tuberculosis</a>, Antimicrobial Agents and Chemotherapy. 2011 Jan | journal-article. doi: 10.1128/AAC.01179-10.

<a href='' target='_blank' class='bux-link'>New analyses of MIC90 data to aid antibacterial drug discovery</a>, MedChemComm. 2011 Jan | journal-article. doi: 10.1039/c1md00095k.

<a href='' target='_blank' class='bux-link'>Pharmacokinetics and Whole‐Blood Bactericidal Activity againstMycobacterium tuberculosisof Single Doses of PNU‐100480 in Healthy Volunteers</a>, The Journal of Infectious Diseases. 2010 Sep | journal-article. doi: 10.1086/655471.

<a href='' target='_blank' class='bux-link'>Structure–activity relationships and hepatic safety risks of thiazole agonists of the thrombopoietin receptor</a>, Bioorganic & Medicinal Chemistry Letters. 2010 Jul | journal-article. doi: 10.1016/j.bmcl.2010.05.087.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-60449113747&partnerID=MN8TOARS' target='_blank' class='bux-link'>The identification of orally bioavailable thrombopoietin agonists</a>, Bioorganic and Medicinal Chemistry Letters. 2009 Jan | journal-article. doi: 10.1016/j.bmcl.2009.01.032.

<a href='' target='_blank' class='bux-link'>The Total Synthesis of the Oxopolyene Macrolide RK-397</a>, Angewandte Chemie. 2007 Feb | journal-article. doi: 10.1002/ange.200602601.

<a href='' target='_blank' class='bux-link'>The Total Synthesis of the Oxopolyene Macrolide RK-397</a>, Angewandte Chemie International Edition. 2007 Feb | journal-article. doi: 10.1002/anie.200602601.

<a href='' target='_blank' class='bux-link'>Chapter 9. Current Approaches to Tuberculosis Drug Discovery and Development</a>, Neglected Diseases and Drug Discovery. 1 Jan | other. doi: 10.1039/9781849733496-00228.

<a href='' target='_blank' class='bux-link'>Diastereoselectivity in the Protonation of Ester Enolates. The Importance of Aggregation with LDA</a>, The Journal of Organic Chemistry. 1995 Jun | journal-article. doi: 10.1021/jo00116a046.

Pui Kai (Tom) Li

Associate Professor

Medicinal Chemistry and Pharmacognosy

Research Areas

Medicinal Chemistry & Pharmacognosy,

Cancer,

Infectious Diseases,

Chemical Synthesis

336 Parks Hall

li.27@osu.edu

(614) 688-0253

Dr. Li’s research interest focuses on the design, syntheses and studies of small molecules for cancers and infectious diseases. In the cancer area, our group focus on prostate and pancreatic cancer. Novel molecules are developed using the strategies of drug repurposing and structure-based drug design (in collaboration with Dr. Xiaolin Cheng). In the research of infectious disease, our focus is on the development of small molecules for the treatment of COVID-19. Novel molecules are generated through computational chemistry, molecular modeling and virtual screening targeting the interface of spike protein and human ACE-2 receptor.

Dr. Li obtained his BS degree in Pharmacy from the University of Wyoming and his Ph.D. in Medicinal Chemistry from The Ohio State University. He conducted his postdoctoral research in the Department of Veterinary Bioscience at The Ohio State University. His first faculty appointment was at the School of Pharmacy, Duquesne University as an assistant professor and then tenured associate professor. In 2000, he joined the Division of Medicinal Chemistry, College of Pharmacy, as tenured associate professor. He was the chair of the division from 2003 to 2013.

1988-1990, Postdoctoral Researcher, Department of Veterinary Biosciences, The Ohio State University

1988, PhD Medicinal Chemistry, The Ohio State University, Medicinal Chemistry

1983, BS Pharmacy, University of Wyoming

1980, University of Nevada, Pre-Pharmacy

1997, Recipient of the Distinguished Research Award, Duquesne University

1997, School of Pharmacy Award for Excellence in Scholarship

1997, President's Award for Excellence

1988, Distinguished Presentation of the 14th annual meeting, Graduate Student Forum, 1988

1987, University Graduate Associate Teaching Award

1983-1984, University Fellowship

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85152339385&partnerID=MN8TOARS' target='_blank' class='bux-link'>BET Bromodomain Inhibitors: Novel Design Strategies and Therapeutic Applications</a>, Molecules. 2023 Jan | journal-article. doi: 10.3390/molecules28073043.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85143088410&partnerID=MN8TOARS' target='_blank' class='bux-link'>Computational modeling studies reveal the origin of the binding preference of 3-(3,4-di hydroisoquinolin-2(1H)-ylsulfonyl)benzoic acids for AKR1C3 over its isoforms</a>, Protein Science. 2022 Jan | journal-article. doi: 10.1002/pro.4499.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85142830989&partnerID=MN8TOARS' target='_blank' class='bux-link'>Constitutively Active Androgen Receptor in Hepatocellular Carcinoma</a>, International Journal of Molecular Sciences. 2022 Jan | journal-article. doi: 10.3390/ijms232213768.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85110642797&partnerID=MN8TOARS' target='_blank' class='bux-link'>ARVib suppresses growth of advanced prostate cancer via inhibition of androgen receptor signaling</a>, Oncogene. 2021 Jan | journal-article. doi: 10.1038/s41388-021-01914-2.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85115753027&partnerID=MN8TOARS' target='_blank' class='bux-link'>Development of Murine Leukemia Virus Integrase-Derived Peptides That Bind Brd4 Extra-Terminal Domain as Candidates for Suppression of Acute Myeloid Leukemia</a>, ACS Pharmacology and Translational Science. 2021 Jan | journal-article. doi: 10.1021/acsptsci.1c00159.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85110387362&partnerID=MN8TOARS' target='_blank' class='bux-link'>Mechanistic Insights into the Allosteric Inhibition of Androgen Receptors by Binding Function 3 Antagonists from an Integrated Molecular Modeling Study</a>, Journal of Chemical Information and Modeling. 2021 Jan | journal-article. doi: 10.1021/acs.jcim.1c00124.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85099100915&partnerID=MN8TOARS' target='_blank' class='bux-link'>Rationally Designed ACE2-Derived Peptides Inhibit SARS-CoV-2</a>, Bioconjugate Chemistry. 2021 Jan | journal-article. doi: 10.1021/acs.bioconjchem.0c00664.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85086566752&partnerID=MN8TOARS' target='_blank' class='bux-link'>A computational study of effects on membrane recruitment of the polar linkers in Vitamin E derivatives</a>, Biochimica et Biophysica Acta - General Subjects. 2020 Jan | journal-article. doi: 10.1016/j.bbagen.2020.129655.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85101356383&partnerID=MN8TOARS' target='_blank' class='bux-link'>Steroid sulfatase stimulates intracrine androgen synthesis and is a therapeutic target for advanced prostate cancer</a>, Clinical Cancer Research. 2020 Jan | journal-article. doi: 10.1158/1078-0432.CCR-20-1682.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85045193288&partnerID=MN8TOARS' target='_blank' class='bux-link'>Correction: Niclosamide and its analogs are potent inhibitors of Wnt/β-catenin, mTOR and STAT3 signaling in ovarian cancer [Oncotarget., 7, (2016) (86803-86815)] 10.18632/oncotarget.13466</a>, Oncotarget. 2018 Jan | journal-article. doi: 10.18632/oncotarget.25151.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85062592979&partnerID=MN8TOARS' target='_blank' class='bux-link'>Therapeutic effects of a novel phenylphthalimide analog for corneal neovascularization and retinal vascular leakage</a>, Investigative Ophthalmology and Visual Science. 2018 Jan | journal-article. doi: 10.1167/IOVS.18-24015.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85014106617&partnerID=MN8TOARS' target='_blank' class='bux-link'>Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer</a>, Bioorganic and Medicinal Chemistry. 2017 Jan | journal-article. doi: 10.1016/j.bmc.2017.02.030.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85019724478&partnerID=MN8TOARS' target='_blank' class='bux-link'>Structure-activity relationship of niclosamide derivatives</a>, Anticancer Research. 2017 Jan | journal-article. doi: 10.21873/anticanres.11635.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85007452262&partnerID=MN8TOARS' target='_blank' class='bux-link'>Niclosamide and its analogs are potent inhibitors of Wnt/ß- catenin, mTOR and STAT3 signaling in ovarian cancer</a>, Oncotarget. 2016 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84994580422&partnerID=MN8TOARS' target='_blank' class='bux-link'>Protective effect of suppressing STAT3 activity in LPS-induced acute lung injury</a>, American Journal of Physiology - Lung Cellular and Molecular Physiology. 2016 Jan | journal-article. doi: 10.1152/ajplung.00281.2016.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84996536976&partnerID=MN8TOARS' target='_blank' class='bux-link'>STAT3 as a potential therapeutic target in ALDH+ and CD44+/CD24+ stem cell-like pancreatic cancer cells</a>, International Journal of Oncology. 2016 Jan | journal-article. doi: 10.3892/ijo.2016.3728.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84943149920&partnerID=MN8TOARS' target='_blank' class='bux-link'>Niclosamide analogs for treatment of ovarian cancer</a>, International Journal of Gynecological Cancer. 2015 Jan | conference-paper. doi: 10.1097/IGC.0000000000000506.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84920384133&partnerID=MN8TOARS' target='_blank' class='bux-link'>Oncolytic potential of a novel KGFR tyrosine kinase inhibitor using a KGFR-selective breast cancer xenograft model</a>, Anticancer Research. 2015 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84901011400&partnerID=MN8TOARS' target='_blank' class='bux-link'>Multi-targeted therapy of cancer by niclosamide: A new application for an old drug</a>, Cancer Letters. 2014 Jan | journal-article. doi: 10.1016/j.canlet.2014.04.003.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84901003920&partnerID=MN8TOARS' target='_blank' class='bux-link'>Pro-growth role of the JMJD2C histone demethylase in HCT-116 colon cancer cells and identification of curcuminoids as JMJD2 inhibitors</a>, American Journal of Translational Research. 2014 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84894274842&partnerID=MN8TOARS' target='_blank' class='bux-link'>Tumor-induced STAT3 signaling in myeloid cells impairs dendritic cell generation by decreasing PKCβII abundance</a>, Science Signaling. 2014 Jan | journal-article. doi: 10.1126/scisignal.2004656.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84879696191&partnerID=MN8TOARS' target='_blank' class='bux-link'>Anticancer activity and SAR studies of substituted 1,4-naphthoquinones</a>, Bioorganic and Medicinal Chemistry. 2013 Jan | journal-article. doi: 10.1016/j.bmc.2013.05.017.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84888857573&partnerID=MN8TOARS' target='_blank' class='bux-link'>Antiproliferative activities and SAR studies of substituted anthraquinones and 1,4-naphthoquinones</a>, Bioorganic and Medicinal Chemistry Letters. 2013 Jan | journal-article. doi: 10.1016/j.bmcl.2013.09.098.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84883489537&partnerID=MN8TOARS' target='_blank' class='bux-link'>Design, synthesis and biological studies of Survivin Dimerization Modulators that prolong mitotic cycle</a>, Bioorganic and Medicinal Chemistry Letters. 2013 Jan | journal-article. doi: 10.1016/j.bmcl.2013.07.034.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84879685991&partnerID=MN8TOARS' target='_blank' class='bux-link'>Design, synthesis and biological studies of novel tubulin inhibitors</a>, Bioorganic and Medicinal Chemistry Letters. 2013 Jan | journal-article. doi: 10.1016/j.bmcl.2013.04.078.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84893511414&partnerID=MN8TOARS' target='_blank' class='bux-link'>Evaluation of STAT3 signaling in ALDH+ and ALDH+/CD44+/CD24- subpopulations of breast cancer cells</a>, PLoS ONE. 2013 Jan | journal-article. doi: 10.1371/journal.pone.0082821.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84874613519&partnerID=MN8TOARS' target='_blank' class='bux-link'>Inhibition of human γ -glutamyl transpeptidase: Development of more potent, physiologically relevant, uncompetitive inhibitors</a>, Biochemical Journal. 2013 Jan | journal-article. doi: 10.1042/BJ20121435.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84882714320&partnerID=MN8TOARS' target='_blank' class='bux-link'>JAK-STAT blockade inhibits tumor initiation and clonogenic recovery of prostate cancer stem-like cells</a>, Cancer Research. 2013 Jan | journal-article. doi: 10.1158/0008-5472.CAN-13-0874.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84886097896&partnerID=MN8TOARS' target='_blank' class='bux-link'>Phosphoproteomic analysis of anaplastic lymphoma kinase (ALK) downstream signaling pathways identifies signal transducer and activator of transcription 3 as a functional target of activated ALK in neuroblastoma cells</a>, FEBS Journal. 2013 Jan | conference-paper. doi: 10.1111/febs.12453.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84888859456&partnerID=MN8TOARS' target='_blank' class='bux-link'>Structure-activity relationship studies of thalidomide analogs with a taxol-like mode of action</a>, Bioorganic and Medicinal Chemistry Letters. 2013 Jan | journal-article. doi: 10.1016/j.bmcl.2013.09.084.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84856099993&partnerID=MN8TOARS' target='_blank' class='bux-link'>A small molecule, LLL12 inhibits constitutive STAT3 and IL-6-induced STAT3 signaling and exhibits potent growth suppressive activity in human multiple myeloma cells</a>, International Journal of Cancer. 2012 Jan | journal-article. doi: 10.1002/ijc.26152.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84864069695&partnerID=MN8TOARS' target='_blank' class='bux-link'>Divergent effects of compounds on the hydrolysis and transpeptidation reactions of γ-glutamyl transpeptidase</a>, Journal of Enzyme Inhibition and Medicinal Chemistry. 2012 Jan | journal-article. doi: 10.3109/14756366.2011.597748.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84866254673&partnerID=MN8TOARS' target='_blank' class='bux-link'>First-in-human trial of a STAT3 decoy oligonucleotide in head and neck tumors: Implications for cancer therapy</a>, Cancer Discovery. 2012 Jan | journal-article. doi: 10.1158/2159-8290.CD-12-0191.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84864350035&partnerID=MN8TOARS' target='_blank' class='bux-link'>Small molecules, LLL12 and FLLL32, inhibit STAT3 and exhibit potent growth suppressive activity in osteosarcoma cells and tumor growth in mice</a>, Investigational New Drugs. 2012 Jan | journal-article. doi: 10.1007/s10637-011-9645-1.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84864996651&partnerID=MN8TOARS' target='_blank' class='bux-link'>Structurally modified curcumin analogs inhibit STAT3 phosphorylation and promote apoptosis of human renal cell carcinoma and melanoma cell lines</a>, PLoS ONE. 2012 Jan | journal-article. doi: 10.1371/journal.pone.0040724.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84868333046&partnerID=MN8TOARS' target='_blank' class='bux-link'>The effect of the steroid sulfatase inhibitor (p-O-sulfamoyl)-tetradecanoyl tyramine (DU-14) on learning and memory in rats with selective lesion of septal-hippocampal cholinergic tract</a>, Neurobiology of Learning and Memory. 2012 Jan | journal-article. doi: 10.1016/j.nlm.2012.09.003.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-80052783097&partnerID=MN8TOARS' target='_blank' class='bux-link'>Creating diverse target-binding surfaces on FKBP12: Synthesis and evaluation of a rapamycin analogue library</a>, ACS Combinatorial Science. 2011 Jan | journal-article. doi: 10.1021/co200057n.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-80053439903&partnerID=MN8TOARS' target='_blank' class='bux-link'>Glioma cell migration on three-dimensional nanofiber scaffolds is regulated by substrate topography and abolished by inhibition of STAT3 signaling</a>, Neoplasia. 2011 Jan | journal-article. doi: 10.1593/neo.11612.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-79960441976&partnerID=MN8TOARS' target='_blank' class='bux-link'>LLL12 inhibits endogenous and exogenous interleukin-6-induced STAT3 phosphorylation in human pancreatic cancer cells</a>, Anticancer Research. 2011 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-82655189564&partnerID=MN8TOARS' target='_blank' class='bux-link'>STAT3 is necessary for proliferation and survival in colon cancer-initiating cells</a>, Cancer Research. 2011 Jan | journal-article. doi: 10.1158/0008-5472.CAN-10-4660.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-79960276970&partnerID=MN8TOARS' target='_blank' class='bux-link'>Targeting colon cancer stem cells using a new curcumin analogue, GO-Y030</a>, British Journal of Cancer. 2011 Jan | journal-article. doi: 10.1038/bjc.2011.200.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-79953112475&partnerID=MN8TOARS' target='_blank' class='bux-link'>The novel curcumin analog FLLL32 decreases STAT3 DNA binding activity and expression, and induces apoptosis in osteosarcoma cell lines</a>, BMC Cancer. 2011 Jan | journal-article. doi: 10.1186/1471-2407-11-112.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-79955416812&partnerID=MN8TOARS' target='_blank' class='bux-link'>The small molecule, lll12, inhibits stat3 phosphorylation and induces apoptosis in medulloblastoma and glioblastoma cells</a>, PLoS ONE. 2011 Jan | journal-article. doi: 10.1371/journal.pone.0018820.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-78650824204&partnerID=MN8TOARS' target='_blank' class='bux-link'>Two small molecule compounds, LLL12 and FLLL32, exhibit potent inhibitory activity on STAT3 in human rhabdomyosarcoma cells</a>, International Journal of Oncology. 2011 Jan | journal-article. doi: 10.3892/ijo-00000848.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-77955520465&partnerID=MN8TOARS' target='_blank' class='bux-link'>A novel small molecule inhibits STAT3 phosphorylation and DNA binding activity and exhibits potent growth suppressive activity in human cancer cells</a>, Molecular Cancer. 2010 Jan | journal-article. doi: 10.1186/1476-4598-9-217.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-73949111590&partnerID=MN8TOARS' target='_blank' class='bux-link'>A novel small molecule, LLL12, inhibits STAT3 phosphorylation and activities and exhibits potent growth-suppressive activity in human cancer cells</a>, Neoplasia. 2010 Jan | journal-article. doi: 10.1593/neo.91196.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-79251479058&partnerID=MN8TOARS' target='_blank' class='bux-link'>Biological activity of 1-aryl-3-phenethylamino-1-propanone hydrochlorides and 3-aroyl-4-aryl-1-phenethyl-4-piperidinols on pc-3 cells and DNA topoisomerase I enzyme</a>, Zeitschrift fur Naturforschung - Section C Journal of Biosciences. 2010 Jan | journal-article. doi: 10.1515/znc-2010-11-1203.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-78751549595&partnerID=MN8TOARS' target='_blank' class='bux-link'>Influence of novel KGFR tyrosine kinase inhibitors on KGF-mediated proliferation of breast cancer</a>, Anticancer Research. 2010 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-77956238512&partnerID=MN8TOARS' target='_blank' class='bux-link'>Inhibition of STAT3 signaling blocks the anti-apoptotic activity of IL-6 in human liver cancer cells</a>, Journal of Biological Chemistry. 2010 Jan | journal-article. doi: 10.1074/jbc.M110.142752.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-78649490370&partnerID=MN8TOARS' target='_blank' class='bux-link'>Investigation of the potential utility of a linomide analogue for treatment of choroidal neovascularization</a>, Experimental Eye Research. 2010 Jan | journal-article. doi: 10.1016/j.exer.2010.10.013.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-77950190311&partnerID=MN8TOARS' target='_blank' class='bux-link'>Novel STAT3 phosphorylation inhibitors exhibit potent growth-suppressive activity in pancreatic and breast cancer cells</a>, Cancer Research. 2010 Jan | journal-article. doi: 10.1158/0008-5472.CAN-09-2468.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84984559474&partnerID=MN8TOARS' target='_blank' class='bux-link'>Sorafenib overcomes TRAIL resistance of hepatocellular carcinoma cells through the inhibition of STAT3</a>, Clinical Cancer Research. 2010 Jan | journal-article. doi: 10.1158/1078-0432.CCR-09-3389.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-77954613878&partnerID=MN8TOARS' target='_blank' class='bux-link'>The small molecule curcumin analog FLLL32 induces apoptosis in melanoma cells via STAT3 inhibition and retains the cellular response to cytokines with anti-tumor activity</a>, Molecular Cancer. 2010 Jan | journal-article. doi: 10.1186/1476-4598-9-165.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-68749089715&partnerID=MN8TOARS' target='_blank' class='bux-link'>Anti-angiogenic and vascular disrupting effects of C9, a new microtubule-depolymerizing agent</a>, British Journal of Pharmacology. 2009 Jan | journal-article. doi: 10.1111/j.1476-5381.2009.00112.x.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-64849088550&partnerID=MN8TOARS' target='_blank' class='bux-link'>Characterization of STAT3 activation and expression in canine and human osteosarcoma</a>, BMC Cancer. 2009 Jan | journal-article. doi: 10.1186/1471-2407-9-81.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-67249125471&partnerID=MN8TOARS' target='_blank' class='bux-link'>Curcumin analogues exhibit enhanced growth suppressive activity in human pancreatic cancer cells</a>, Anti-Cancer Drugs. 2009 Jan | journal-article. doi: 10.1097/CAD.0b013e32832afc04.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-58549094898&partnerID=MN8TOARS' target='_blank' class='bux-link'>Curcumin is a potent DNA hypomethylation agent</a>, Bioorganic and Medicinal Chemistry Letters. 2009 Jan | journal-article. doi: 10.1016/j.bmcl.2008.12.041.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-58149267888&partnerID=MN8TOARS' target='_blank' class='bux-link'>LLL-3 inhibits STAT3 activity, suppresses glioblastoma cell growth and prolongs survival in a mouse glioblastoma model</a>, British Journal of Cancer. 2009 Jan | journal-article. doi: 10.1038/sj.bjc.6604793.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-65649091667&partnerID=MN8TOARS' target='_blank' class='bux-link'>Modulation of DNA methylation by a sesquiterpene lactone parthenolide</a>, Journal of Pharmacology and Experimental Therapeutics. 2009 Jan | journal-article. doi: 10.1124/jpet.108.147934.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-70149085608&partnerID=MN8TOARS' target='_blank' class='bux-link'>New curcumin analogues exhibit enhanced growth-suppressive activity and inhibit AKT and signal transducer and activator of transcription 3 phosphorylation in breast and prostate cancer cells</a>, Cancer Science. 2009 Jan | journal-article. doi: 10.1111/j.1349-7006.2009.01220.x.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-65149101403&partnerID=MN8TOARS' target='_blank' class='bux-link'>New structural analogues of curcumin exhibit potent growth suppressive activity in human colorectal carcinoma cells</a>, BMC Cancer. 2009 Jan | journal-article. doi: 10.1186/1471-2407-9-99.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-61849139127&partnerID=MN8TOARS' target='_blank' class='bux-link'>Structure-activity relationship studies of curcumin analogues</a>, Bioorganic and Medicinal Chemistry Letters. 2009 Jan | journal-article. doi: 10.1016/j.bmcl.2009.01.104.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-37549062631&partnerID=MN8TOARS' target='_blank' class='bux-link'>Design, synthesis, and studies of small molecule STAT3 inhibitors</a>, Bioorganic and Medicinal Chemistry Letters. 2008 Jan | journal-article. doi: 10.1016/j.bmcl.2007.10.031.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-57349147068&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and cytotoxicity of novel 3-aryl-1-(3′-dibenzylaminomethyl- 4′-hydroxyphenyl)-propenones and related compounds</a>, Chemical and Pharmaceutical Bulletin. 2008 Jan | journal-article. doi: 10.1248/cpb.56.1675.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-35748960845&partnerID=MN8TOARS' target='_blank' class='bux-link'>A novel steroidal selective steroid sulfatase inhibitor KW-2581 inhibits sulfated-estrogen dependent growth of breast cancer cells in vitro and in animal models</a>, Breast Cancer Research and Treatment. 2007 Jan | journal-article. doi: 10.1007/s10549-007-9495-x.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-37549000113&partnerID=MN8TOARS' target='_blank' class='bux-link'>Development of keratinocyte growth factor receptor tyrosine kinase inhibitors for the treatment of cancer</a>, Anticancer Research. 2007 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-34547699257&partnerID=MN8TOARS' target='_blank' class='bux-link'>Immunohistochemical analysis of steroid sulfatase in human tissues</a>, Journal of Steroid Biochemistry and Molecular Biology. 2007 Jan | journal-article. doi: 10.1016/j.jsbmb.2006.12.105.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-34447558569&partnerID=MN8TOARS' target='_blank' class='bux-link'>Inhibition of steroid sulfatase activity and cell proliferation in ZR-75-1 and BT-474 human breast cancer cells by KW-2581 in vitro and in vivo</a>, Breast Cancer Research and Treatment. 2007 Jan | journal-article. doi: 10.1007/s10549-006-9404-8.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-34548850889&partnerID=MN8TOARS' target='_blank' class='bux-link'>Inhibitors of NF-κB derived from thalidomide</a>, Bioorganic and Medicinal Chemistry Letters. 2007 Jan | journal-article. doi: 10.1016/j.bmcl.2007.01.088.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-38649125575&partnerID=MN8TOARS' target='_blank' class='bux-link'>Keratinocyte growth factor receptor tyrosine kinase antagonists for the prevention of metastatic cancer progression</a>, Drugs of the Future. 2007 Jan | journal-article. doi: 10.1358/dof.2007.032.11.1131966.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-34250861273&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of 4′-hydroxy-3′-piperidinomethylchalcone derivatives and their cytotoxicity against PC-3 cell lines</a>, Archiv der Pharmazie. 2007 Jan | journal-article. doi: 10.1002/ardp.200600072.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33644983367&partnerID=MN8TOARS' target='_blank' class='bux-link'>A thalidomide analogue with in vitro antiproliferative, antimitotic, and microtubule-stabilizing activities</a>, Molecular Cancer Therapeutics. 2006 Jan | journal-article. doi: 10.1158/1535-7163.MCT-05-0254.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33845915669&partnerID=MN8TOARS' target='_blank' class='bux-link'>Evaluation of the cytotoxicity of some mono-Mannich bases and their corresponding azine derivatives against androgen-independent prostate cancer cells</a>, Arzneimittel-Forschung/Drug Research. 2006 Jan | journal-article. doi: 10.1055/s-0031-1296797.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33747199112&partnerID=MN8TOARS' target='_blank' class='bux-link'>Structure-activity-relationship studies of conformationally restricted analogs of combretastatin A-4 derived from SU5416</a>, Bioorganic and Medicinal Chemistry. 2006 Jan | journal-article. doi: 10.1016/j.bmc.2006.06.017.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-27644444372&partnerID=MN8TOARS' target='_blank' class='bux-link'>Conformationally restricted analogs of Combretastatin A-4 derived from SU5416</a>, Bioorganic and Medicinal Chemistry Letters. 2005 Jan | journal-article. doi: 10.1016/j.bmcl.2005.09.001.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-19344369223&partnerID=MN8TOARS' target='_blank' class='bux-link'>Erratum: The actions of a charged melatonin receptor ligand, TMEPI, and an irreversible MT2 receptor agonist, BMNEP, on mouse hippocampal evoked potentials in vitro (Life Sciences (2004) 75 (3147-3156) DOI: 10.1016/j.lfs.2004.06.009)</a>, Life Sciences. 2005 Jan | journal-article. doi: 10.1016/j.lfs.2005.01.006.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-14744300170&partnerID=MN8TOARS' target='_blank' class='bux-link'>Neurosteroid paradoxical enhancement of paired-pulse inhibition through paired-pulse facilitation of inhibitory circuits in dentate granule cells</a>, Neuropharmacology. 2005 Jan | journal-article. doi: 10.1016/j.neuropharm.2004.11.014.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-23744462619&partnerID=MN8TOARS' target='_blank' class='bux-link'>Translational studies on aromatase, cyclooxygenases, and enzyme inhibitors in breast cancer</a>, Journal of Steroid Biochemistry and Molecular Biology. 2005 Jan | conference-paper. doi: 10.1016/j.jsbmb.2005.04.013.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-4544269063&partnerID=MN8TOARS' target='_blank' class='bux-link'>Fetal alcohol exposure alters neurosteroid levels in the developing rat brain</a>, Journal of Neurochemistry. 2004 Jan | journal-article. doi: 10.1111/j.1471-4159.2004.02686.x.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-3342985840&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of new estrone derivatives using excess oxalyl chloride</a>, Chemistry of Natural Compounds. 2004 Jan | journal-article. doi: 10.1023/B:CONC.0000025465.76505.33.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-5444233014&partnerID=MN8TOARS' target='_blank' class='bux-link'>The actions of a charged melatonin receptor ligand, TMEPI, and an irreversible MT2 receptor agonist, BMNEP, on mouse hippocampal evoked potentials in vitro</a>, Life Sciences. 2004 Jan | journal-article. doi: 10.1016/j.lfs.2004.06.009.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-10744226017&partnerID=MN8TOARS' target='_blank' class='bux-link'>Role of steroid sulfatase in local formation of estrogen in post-menopausal breast cancer patients</a>, Journal of Steroid Biochemistry and Molecular Biology. 2003 Jan | conference-paper. doi: 10.1016/S0960-0760(03)00357-1.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0037463778&partnerID=MN8TOARS' target='_blank' class='bux-link'>Structure-activity relationships studies of the anti-angiogenic activities of linomide</a>, Bioorganic and Medicinal Chemistry Letters. 2003 Jan | journal-article. doi: 10.1016/S0960-894X(03)00047-7.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0036579909&partnerID=MN8TOARS' target='_blank' class='bux-link'>Effects of putative hydroxylated thalidomide metabolites on blood vessel density in the chorioallantoic membrane (CAM) assay and on tumor and endothelial cell proliferation</a>, Biological and Pharmaceutical Bulletin. 2002 Jan | journal-article. doi: 10.1248/bpb.25.597.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0036753565&partnerID=MN8TOARS' target='_blank' class='bux-link'>Inhibition of steryl sulfatase activity in LNCaP human prostate cancer cells</a>, Steroids. 2002 Jan | journal-article. doi: 10.1016/S0039-128X(02)00030-2.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0036511701&partnerID=MN8TOARS' target='_blank' class='bux-link'>Solid-phase synthesis of thalidomide and its analogues</a>, Journal of Combinatorial Chemistry. 2002 Jan | journal-article. doi: 10.1021/cc010038n.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0036482542&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and pharmacological analysis of high affinity melatonin receptor ligands</a>, Chemical and Pharmaceutical Bulletin. 2002 Jan | journal-article. doi: 10.1248/cpb.50.272.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0035814077&partnerID=MN8TOARS' target='_blank' class='bux-link'>Design and synthesis of Pfmrk inhibitors as potential antimalarial agents</a>, Bioorganic and medicinal chemistry letters. 2001 Jan | journal-article. doi: 10.1016/S0960-894X(01)00578-9.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0035862425&partnerID=MN8TOARS' target='_blank' class='bux-link'>N1E-115 mouse neuroblastoma cells express mt1 melatonin receptors and produce neurites in response to melatonin</a>, Biochimica et Biophysica Acta - Molecular Cell Research. 2001 Jan | journal-article. doi: 10.1016/S0167-4889(00)00127-0.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0035014598&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of naphthalenic melatonin receptor ligands</a>, Synthetic Communications. 2001 Jan | journal-article. doi: 10.1081/SCC-100000591.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0033631480&partnerID=MN8TOARS' target='_blank' class='bux-link'>Melatonin receptors and ligands</a>, Vitamins and Hormones. 2000 Jan | book. doi: 10.1016/s0083-6729(00)58030-3.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0033740169&partnerID=MN8TOARS' target='_blank' class='bux-link'>Melatonin receptors as potential targets for drug discovery</a>, Drugs of the Future. 2000 Jan | journal-article. doi: 10.1358/dof.2000.025.09.858694.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0034739790&partnerID=MN8TOARS' target='_blank' class='bux-link'>Steroid sulfatase activity in the rat ovary, cultured granulosa cells, and a granulosa cell line</a>, Journal of Steroid Biochemistry and Molecular Biology. 2000 Jan | journal-article. doi: 10.1016/S0960-0760(00)00171-0.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0034210885&partnerID=MN8TOARS' target='_blank' class='bux-link'>Steroid sulfatase inhibitor alters blood pressure and steroid profiles in hypertensive rats</a>, Journal of Steroid Biochemistry and Molecular Biology. 2000 Jan | journal-article. doi: 10.1016/S0960-0760(00)00062-5.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0034085681&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of [25,26,26,26,27,27,27-d7]-cholesterol</a>, Journal of Labelled Compounds and Radiopharmaceuticals. 2000 Jan | journal-article. doi: 10.1002/1099-1344(200007)43:8<773::AID-JLCR361>3.0.CO;2-G.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0034716954&partnerID=MN8TOARS' target='_blank' class='bux-link'>The effect of steroid sulfatase inhibition on learning and spatial memory</a>, Brain Research. 2000 Jan | journal-article. doi: 10.1016/S0006-8993(00)02372-6.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0033734746&partnerID=MN8TOARS' target='_blank' class='bux-link'>Tissue steroid sulfatase levels, testosterone and blood pressure</a>, Journal of Steroid Biochemistry and Molecular Biology. 2000 Jan | journal-article. doi: 10.1016/S0960-0760(00)00075-3.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0033062017&partnerID=MN8TOARS' target='_blank' class='bux-link'>Development of (p-O-sulfamoyl)-N-alkanoyl-phenylalkyl amines as non- steroidal estrone sulfatase inhibitors</a>, Journal of Steroid Biochemistry and Molecular Biology. 1999 Jan | journal-article. doi: 10.1016/S0960-0760(98)00159-9.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0032870870&partnerID=MN8TOARS' target='_blank' class='bux-link'>Peripheral steroid sulfatase inhibition potentiates improvement of memory retention for hippocampally administered dehydroepiandrosterone sulfate but not pregnenolone sulfate</a>, Psychoneuroendocrinology. 1999 Jan | journal-article. doi: 10.1016/S0306-4530(99)00030-X.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0033579859&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and sulfatase inhibitory activities of (E)- and (Z)-4- hydroxytamoxifen sulfamates</a>, Bioorganic and Medicinal Chemistry Letters. 1999 Jan | journal-article. doi: 10.1016/S0960-894X(98)00707-0.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0031842368&partnerID=MN8TOARS' target='_blank' class='bux-link'>Development of potent non-estrogenic estrone sulfatase inhibitors</a>, Steroids. 1998 Jan | journal-article. doi: 10.1016/S0039-128X(98)00044-0.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0032055392&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of 17-oxoandrosta-3,5-dien-3-methyl sulfonate as stable analog of dehydroepiandrosterone sulfate</a>, Steroids. 1998 Jan | journal-article. doi: 10.1016/S0039-128X(98)00006-3.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0031966026&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of a radiolabeled charged melatonin receptor ligand</a>, Journal of Labelled Compounds and Radiopharmaceuticals. 1998 Jan | journal-article. doi: 10.1002/(SICI)1099-1344(199805)41:5<435::AID-JLCR97>3.0.CO;2-L.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0342981444&partnerID=MN8TOARS' target='_blank' class='bux-link'>Chronic steroid sulfatase inhibition by (p-o-sulfamoyl)-N-tetradecanoyl tyramine increases dehydroepiandrosterone sulfate in whole brain</a>, Life Sciences. 1997 Jan | journal-article. doi: 10.1016/S0024-3205(97)00961-2.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0031578626&partnerID=MN8TOARS' target='_blank' class='bux-link'>Development of a high-affinity ligand that binds irreversibly to Mel1b melatonin receptors.</a>, Journal of medicinal chemistry. 1997 Jan | journal-article. doi: 10.1021/jm970437q.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0030671365&partnerID=MN8TOARS' target='_blank' class='bux-link'>Enhanced plasma DHEAS, brain acetylcholine and memory mediated by steroid sulfatase inhibition</a>, Brain Research. 1997 Jan | journal-article. doi: 10.1016/S0006-8993(97)00867-6.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0031045478&partnerID=MN8TOARS' target='_blank' class='bux-link'>Inhibition of estrone sulfatase and proliferation of human breast cancer cells by nonsteroidal (p-O-sulfamoyl)-N-alkanoyl tyramines</a>, Cancer Research. 1997 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0030764441&partnerID=MN8TOARS' target='_blank' class='bux-link'>Structure-activity relationship studies of the amide functionality in (p-O-sulfamoyl)-N-alkanoyl tyramines as estrone sulfatase inhibitors</a>, Steroids. 1997 Jan | journal-article. doi: 10.1016/S0039-128X(97)00038-X.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0030967890&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and receptor binding studies of quinolinic derivatives as melatonin receptor ligands</a>, Bioorganic and Medicinal Chemistry Letters. 1997 Jan | journal-article. doi: 10.1016/S0960-894X(97)00392-2.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0030797198&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis of sodium androst-5-ene-17-one 3β methylene sulfonate</a>, Steroids. 1997 Jan | journal-article. doi: 10.1016/S0039-128X(97)00039-1.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0030799248&partnerID=MN8TOARS' target='_blank' class='bux-link'>The development of a charged melatonin receptor ligand</a>, Bioorganic and Medicinal Chemistry Letters. 1997 Jan | journal-article. doi: 10.1016/S0960-894X(97)00444-7.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0030590485&partnerID=MN8TOARS' target='_blank' class='bux-link'>Enhancement of hippocampal acetylcholine release by the neurosteroid dehydroepiandrosterone sulfate: An in vivo microdialysis study</a>, Brain Research. 1996 Jan | journal-article. doi: 10.1016/0006-8993(96)00751-2.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33748982661&partnerID=MN8TOARS' target='_blank' class='bux-link'>In vivo effects of dehydroepiandrosterone sulfate (dheas) on acetylcholine release in the hippocampus of anesthetized rats</a>, FASEB Journal. 1996 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0030236696&partnerID=MN8TOARS' target='_blank' class='bux-link'>Inhibition of placental estrone sulfatase activity and MCF-7 breast cancer cell proliferation by estrone-3-amino derivatives</a>, Journal of Steroid Biochemistry and Molecular Biology. 1996 Jan | journal-article. doi: 10.1016/S0960-0760(96)00089-1.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0030572961&partnerID=MN8TOARS' target='_blank' class='bux-link'>Memory enhancement mediated by the steroid sulfatase inhibitor (p-O-sulfamoyl)-N-tetradecanoyl tyramine</a>, Life Sciences. 1996 Jan | journal-article. doi: 10.1016/s0024-3205(96)00621-2.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0030238263&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and sulfatase inhibitory activities of non-steroidal estrone sulfatase inhibitors</a>, Journal of Steroid Biochemistry and Molecular Biology. 1996 Jan | journal-article. doi: 10.1016/S0960-0760(96)00093-3.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0028965352&partnerID=MN8TOARS' target='_blank' class='bux-link'>Estrogenicity, antiestrogenicity and estrone sulfatase inhibition of estrone-3-amine and estrone-3-thiol</a>, Journal of Steroid Biochemistry and Molecular Biology. 1995 Jan | journal-article. doi: 10.1016/0960-0760(94)00176-M.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0028948089&partnerID=MN8TOARS' target='_blank' class='bux-link'>Estrone sulfate analogs as estrone sulfatase inhibitors</a>, Steroids. 1995 Jan | journal-article. doi: 10.1016/0039-128X(94)00048-H.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0028800150&partnerID=MN8TOARS' target='_blank' class='bux-link'>Reversal of scopolamine induced amnesia in rats by the steroid sulfatase inhibitor estrone-3-O-sulfamate</a>, Cognitive Brain Research. 1995 Jan | journal-article. doi: 10.1016/0926-6410(95)90016-0.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0028060415&partnerID=MN8TOARS' target='_blank' class='bux-link'>Inhibition of human placental sterylsulfatase by synthetic analogs of estrone sulfate</a>, Journal of Steroid Biochemistry and Molecular Biology. 1994 Jan | journal-article. doi: 10.1016/0960-0760(94)90130-9.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0027325184&partnerID=MN8TOARS' target='_blank' class='bux-link'>In vitro uptake and autoradiographic localization of tritiated gossypol in Taenia taeniaeformis metacestodes</a>, Parasitology Research. 1993 Jan | journal-article. doi: 10.1007/BF00932182.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0027399723&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and biochemical studies of estrone sulfatase inhibitors</a>, Steroids. 1993 Jan | journal-article. doi: 10.1016/0039-128X(93)90045-O.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0026541676&partnerID=MN8TOARS' target='_blank' class='bux-link'>Aromatase inhibition by 7-substituted steroids in human choriocarcinoma cell culture</a>, Journal of Steroid Biochemistry and Molecular Biology. 1992 Jan | journal-article. doi: 10.1016/0960-0760(92)90228-B.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0026716047&partnerID=MN8TOARS' target='_blank' class='bux-link'>Characteristics of covalent gossypol binding to microsomal proteins</a>, Research Communications in Chemical Pathology and Pharmacology. 1992 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0025869306&partnerID=MN8TOARS' target='_blank' class='bux-link'>Gossypolone suppresses progesterone synthesis in bovine luteal cells</a>, Journal of Steroid Biochemistry and Molecular Biology. 1991 Jan | journal-article. doi: 10.1016/0960-0760(91)90082-G.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0025063838&partnerID=MN8TOARS' target='_blank' class='bux-link'>7-Substituted 1,4,6-androstatriene-3,17-diones as enzyme-activated irreversible inhibitors of aromatase</a>, Journal of Steroid Biochemistry. 1990 Jan | journal-article. doi: 10.1016/0022-4731(90)90170-W.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0025673957&partnerID=MN8TOARS' target='_blank' class='bux-link'>7-substituted steroidal aromatase inhibitors: Structure-activity relationships and molecular modeling</a>, Journal of Enzyme Inhibition and Medicinal Chemistry. 1990 Jan | journal-article. doi: 10.3109/14756369009040732.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0025649142&partnerID=MN8TOARS' target='_blank' class='bux-link'>Biochemical and pharmacological development of steroidal inhibitors of aromatase</a>, Journal of Steroid Biochemistry and Molecular Biology. 1990 Jan | journal-article. doi: 10.1016/0960-0760(90)90488-7.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-77956894005&partnerID=MN8TOARS' target='_blank' class='bux-link'>Diclofenac Sodium</a>, Analytical Profiles of Drug Substances and Excipients. 1990 Jan | book. doi: 10.1016/S0099-5428(08)60366-4.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0025099480&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and Biochemical Studies of 7-Substituted 4,6-Androstadiene-3,17-diones as Aromatase Inhibitors</a>, Journal of Medicinal Chemistry. 1990 Jan | journal-article. doi: 10.1021/jm00163a017.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0024272363&partnerID=MN8TOARS' target='_blank' class='bux-link'>Effects of the aromatase inhibitor 7α-(4' -amino)phenylthio-4-androstene-3, 17-dione on 7, 12-dimethylbenz(a)anthracene-induced mammary carcinoma in rats</a>, Cancer Research. 1988 Jan | journal-article. .

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0023518823&partnerID=MN8TOARS' target='_blank' class='bux-link'>7 α -Substituted androstenediones as effective in vttro and in vivo inhibitors of aromatase</a>, Steroids. 1987 Jan | journal-article. doi: 10.1016/0039-128X(83)90069-7.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-45949113079&partnerID=MN8TOARS' target='_blank' class='bux-link'>7α-substituted steroidal aromatase inhibitors in hormone-dependent breast cancer in culture and in vivo [Poster 23]</a>, Steroids. 1987 Jan | journal-article. doi: 10.1016/0039-128x(87)90064-x.

Kou-San Ju

Assistant Professor

Medicinal Chemistry and Pharmacognosy

Research Areas

Medicinal Chemistry & Pharmacognosy,

Central Nervous System Disorders,

Infectious Diseases,

Chemical Biology,

Computational Biomedicine & Data Analytics,

Natural Products

290 Aronoff Laboratory

ju.109@osu.edu

(614) 292-8847

Professional Website

My interdisciplinary research program is inspired by the metabolic diversity of microorganisms and the vast array of compounds they produce. Working at the interface of chemistry and biology, my group combines approaches in chemistry, biochemistry, bioinformatics, genetics, and systems biology to discover new natural products, identify bioactivity and mode of action, and to decipher the metabolic basis of their biosynthesis. Ultimately, we seek to translate insights gained from our investigations into solutions for modern day challenges facing human health and the environment. These include new antibiotics to counter drug-resistant pathogens, novel herbicides and biocontrol agents to improve pest management and food security, and engineered biocatalysts to facilitate chemical production by green chemistry and industrial biotechnology.

Tryon JH, Rote JC, Chen L, Robey MT, Vega MM, Phua WC, Metcalf WW, Ju KS, Kelleher NL, Thomson RJ. Genome Mining and Metabolomics Uncover a Rare d-Capreomycidine Containing Natural Product and Its Biosynthetic Gene Cluster. ACS Chem Biol. 2020 Nov 20;15(11):3013-3020. doi: 10.1021/acschembio.0c00663. Epub 2020 Nov 5. PMID: 33151679; PMCID: PMC7830813.

Kayrouz CM, Zhang Y, Pham TM, Ju KS. Genome Mining Reveals the Phosphonoalamide Natural Products and a New Route in Phosphonic Acid Biosynthesis. ACS Chem Biol. 2020 Jul 17;15(7):1921-1929. doi: 10.1021/acschembio.0c00256. Epub 2020 Jun 15. PMID: 32484327.

Parkinson EI, Erb A, Eliot AC, Ju KS, Metcalf WW. Fosmidomycin biosynthesis diverges from related phosphonate natural products. Nat Chem Biol. 2019 Nov;15(11):1049-1056. doi: 10.1038/s41589-019-0343-1. Epub 2019 Aug 26. PMID: 31451762; PMCID: PMC7098449.

Ali T, Pham TM, Ju KS, Rakotondraibe HL. homocyclopiamine B, a Prenylated Indole Alkaloid of Biogenetic Interest from the Endophytic Fungus Penicillium concentricum. Molecules. 2019 Jan 9;24(2):218. doi: 10.3390/molecules24020218. PMID: 30634398; PMCID: PMC6359132.

Goettge MN, Cioni JP, Ju KS, Pallitsch K, Metcalf WW. PcxL and HpxL are flavin-dependent, oxime-forming N-oxidases in phosphonocystoximic acid biosynthesis in Streptomyces. J Biol Chem. 2018 May 4;293(18):6859-6868. doi: 10.1074/jbc.RA118.001721. Epub 2018 Mar 14. PMID: 29540479; PMCID: PMC5936822.

Ju KS, Zhang X, Elliot MA. New Kid on the Block: LmbU Expands the Repertoire of Specialized Metabolic Regulators in Streptomyces. J Bacteriol. 2017 Dec 20;200(2):e00559-17. doi: 10.1128/JB.00559-17. PMID: 29084856; PMCID: PMC5738733.

Born DA, Ulrich EC, Ju KS, Peck SC, van der Donk WA, Drennan CL. Structural basis for methylphosphonate biosynthesis. Science. 2017 Dec 8;358(6368):1336-1339. doi: 10.1126/science.aao3435. PMID: 29217579; PMCID: PMC5901744.

Amato KR, Ulanov A, Ju KS, Garber PA. Metabolomic data suggest regulation of black howler monkey (Alouatta pigra) diet composition at the molecular level. Am J Primatol. 2017 Apr;79(4):1-10. doi: 10.1002/ajp.22616. Epub 2016 Dec 9. PMID: 27936282.

Labeda DP, Dunlap CA, Rong X, Huang Y, Doroghazi JR, Ju KS, Metcalf WW. Phylogenetic relationships in the family Streptomycetaceae using multi-locus sequence analysis. Antonie Van Leeuwenhoek. 2017 Apr;110(4):563-583. doi: 10.1007/s10482-016-0824-0. Epub 2016 Dec 30. PMID: 28039547.

Freestone TS, Ju KS, Wang B, Zhao H. Discovery of a Phosphonoacetic Acid Derived Natural Product by Pathway Refactoring. ACS Synth Biol. 2017 Feb 17;6(2):217-223. doi: 10.1021/acssynbio.6b00299. Epub 2017 Jan 23. PMID: 28103011.

James Fuchs

Associate Dean for Research and Graduate Studies

Professor

Medicinal Chemistry and Pharmacognosy

College Administration

Research Areas

Cancer,

Infectious Diseases,

Chemical Synthesis,

Natural Products,

Medicinal Chemistry & Pharmacognosy

634 Riffe

fuchs.42@osu.edu

(614) 247-7377

Professional Website

The research in Dr. Fuchs' lab focuses on the design and preparation of bioactive molecules for therapeutic applications against cancer and infectious diseases. His lab utilizes fundamental chemical knowledge and synthetic methodology to facilitate the process of drug discovery and development through the generation of biological probe molecules, the synthesis and modification of lead compounds, and the optimization of drug properties. The overarching goals of these studies are to understand the mechanisms through which small molecules interact with proteins or other biomolecules in the context of disease progression and to improve the potential utility of promising new compounds to help them advance toward the clinic. Recently, the Fuchs lab has collaborated with numerous labs in the areas of natural product drug development for various cancers, the preparation of protein degraders active against leukemia, and HIV-1 capsid and integrase drug development.

2007, Postdoctoral Fellow, The Scripps Research Institute, Medicinal/Organic Chemistry

2005, PhD, Pennsylvania State University, Organic Chemistry

1998, BS, cum laude, University Honors, Honors in Chemistry, University of Toledo, Chemistry

<a href='https://doi.org/10.1021/acsmedchemlett.3c00082' target='_blank' class='bux-link'>Examination of the Impact of Triazole Position within Linkers on Solubility and Lipophilicity of a CDK9 Degrader Series</a>, ACS Medicinal Chemistry Letters. 2023 Jul | journal-article. doi: 10.1021/acsmedchemlett.3c00082.

<a href='https://doi.org/10.1039/d2np00091a' target='_blank' class='bux-link'>Discovery and development of botanical natural products and their analogues as therapeutics for ovarian cancer.</a>, Natural product reports. 2023 Jun | review. doi: 10.1039/d2np00091a.

<a href='https://doi.org/10.1021/acs.molpharmaceut.3c00069' target='_blank' class='bux-link'>Exploration of Verticillins in High-Grade Serous Ovarian Cancer and Evaluation of Multiple Formulations in Preclinical In Vitro and In Vivo Models</a>, Molecular Pharmaceutics. 2023 Jun | journal-article. doi: 10.1021/acs.molpharmaceut.3c00069.

<a href='https://doi.org/10.1038/s42004-023-00897-3' target='_blank' class='bux-link'>G2Retro as a two-step graph generative models for retrosynthesis prediction</a>, Communications Chemistry. 2023 May | journal-article. doi: 10.1038/s42004-023-00897-3.

<a href='https://europepmc.org/articles/PMC9600929' target='_blank' class='bux-link'>Structural and Mechanistic Bases of Viral Resistance to HIV-1 Capsid Inhibitor Lenacapavir.</a>, mBio. 2022 Oct | journal-article. doi: 10.1128/mbio.01804-22.

<a href='https://europepmc.org/articles/PMC9241644' target='_blank' class='bux-link'>Evaluation of Novel Quorum Sensing Inhibitors Targeting Auto-Inducer 2 (AI-2) for the Control of Avian Pathogenic Escherichia coli Infections in Chickens.</a>, Microbiology spectrum. 2022 May | journal-article. doi: 10.1128/spectrum.00286-22.

<a href='https://doi.org/10.1021/acs.jnatprod.2c00036' target='_blank' class='bux-link'>Discovery of Anticancer Agents of Diverse Natural Origin.</a>, Journal of natural products. 2022 Feb | journal-article. doi: 10.1021/acs.jnatprod.2c00036.

<a href='https://doi.org/10.1021/acsomega.1c06378' target='_blank' class='bux-link'>Identification and Optimization of a Novel HIV-1 Integrase Inhibitor</a>, ACS Omega. 2022 Feb | journal-article. doi: 10.1021/acsomega.1c06378.

<a href='http://dx.doi.org/10.1038/s41419-021-04495-w' target='_blank' class='bux-link'>PHY34 inhibits autophagy through V-ATPase V0A2 subunit inhibition and CAS/CSE1L nuclear cargo trafficking in high grade serous ovarian cancer</a>, Cell Death & Disease. 2022 Jan | journal-article. doi: 10.1038/s41419-021-04495-w.

<a href='http://dx.doi.org/10.1007/s12013-021-01030-8' target='_blank' class='bux-link'>Pentalinonsterol, a Phytosterol from Pentalinon andrieuxii, is Immunomodulatory through Phospholipase A2 in Macrophages toward its Antileishmanial Action</a>, Cell Biochemistry and Biophysics. 2021 Aug | journal-article. doi: 10.1007/s12013-021-01030-8.

<a href='https://doi.org/10.1021/acsmedchemlett.1c00024' target='_blank' class='bux-link'>Semisynthetic Derivatives of the Verticillin Class of Natural Products through Acylation of the C11 Hydroxy Group</a>, ACS Medicinal Chemistry Letters. 2021 Apr | journal-article. doi: 10.1021/acsmedchemlett.1c00024.

<a href='http://dx.doi.org/10.1016/j.phytochem.2020.112521' target='_blank' class='bux-link'>Specialized metabolites of the United States lichen Niebla homalea and their antiproliferative activities</a>, Phytochemistry. 2020 Dec | journal-article. doi: 10.1016/j.phytochem.2020.112521.

<a href='http://dx.doi.org/10.1126/science.abb4808' target='_blank' class='bux-link'>Structural and mechanistic bases for a potent HIV-1 capsid
inhibitor</a>, Science. 2020 Oct | journal-article. doi: 10.1126/science.abb4808.

<a href='https://doi.org/10.1021/acschembio.9b00993' target='_blank' class='bux-link'>15N Stable Isotope Labeling and Comparative Metabolomics Facilitates Genome Mining in Cultured Cyanobacteria</a>, ACS Chemical Biology. 2020 Mar | journal-article. doi: 10.1021/acschembio.9b00993.

<a href='https://doi.org/10.1021/acs.jcim.9b00489' target='_blank' class='bux-link'>STarFish: A Stacked Ensemble Target Fishing Approach and its Application to Natural Products</a>, Journal of Chemical Information and Modeling. 2019 Nov | journal-article. doi: 10.1021/acs.jcim.9b00489.

<a href='http://dx.doi.org/10.1016/j.ijpddr.2019.08.004' target='_blank' class='bux-link'>Evaluation of synergy between host and pathogen-directed therapies against intracellular Leishmania donovani</a>, International Journal for Parasitology: Drugs and Drug Resistance. 2019 Aug | journal-article. doi: 10.1016/j.ijpddr.2019.08.004.

<a href='http://dx.doi.org/10.1038/s41429-019-0168-x' target='_blank' class='bux-link'>Novel narrow spectrum benzyl thiophene sulfonamide derivatives to control Campylobacter</a>, The Journal of Antibiotics. 2019 Jul | journal-article. doi: 10.1038/s41429-019-0168-x.

<a href='http://dx.doi.org/10.7554/elife.46344' target='_blank' class='bux-link'>HIV-1 integrase tetramers are the antiviral target of pyridine-based allosteric integrase inhibitors</a>, eLife. 2019 May | journal-article. doi: 10.7554/elife.46344.

<a href='http://dx.doi.org/10.1111/cei.13258' target='_blank' class='bux-link'>Novel small molecule IL-6 inhibitor suppresses autoreactive Th17 development and promotes Treg development</a>, Clinical and Experimental Immunology. 2019 Apr | journal-article. doi: 10.1111/cei.13258.

<a href='https://doi.org/10.1021/acs.jnatprod.9b00018' target='_blank' class='bux-link'>Potential Anticancer Agents Characterized from Selected Tropical Plants</a>, Journal of Natural Products. 2019 Mar | journal-article. doi: 10.1021/acs.jnatprod.9b00018.

<a href='https://doi.org/10.1021/acsmedchemlett.8b00633' target='_blank' class='bux-link'>An Isoquinoline Scaffold as a Novel Class of Allosteric HIV-1 Integrase Inhibitors</a>, ACS Medicinal Chemistry Letters. 2019 Feb | journal-article. doi: 10.1021/acsmedchemlett.8b00633.

<a href='http://dx.doi.org/10.1016/j.chempr.2018.11.007' target='_blank' class='bux-link'>Site-Selective C–H Functionalization of (Hetero)Arenes via Transient, Non-symmetric Iodanes</a>, Chem. 2019 Feb | journal-article. doi: 10.1016/j.chempr.2018.11.007.

<a href='http://dx.doi.org/10.3389/fmicb.2018.02804' target='_blank' class='bux-link'>Identification of a Small Molecule Anti-biofilm Agent Against Salmonella enterica</a>, Frontiers in Microbiology. 2018 Nov | journal-article. doi: 10.3389/fmicb.2018.02804.

<a href='http://dx.doi.org/10.1158/1535-7163.mct-17-1195' target='_blank' class='bux-link'>Phyllanthusmin Derivatives Induce Apoptosis and Reduce Tumor Burden in High-Grade Serous Ovarian Cancer by Late-Stage Autophagy Inhibition</a>, Molecular Cancer Therapeutics. 2018 Oct | journal-article. doi: 10.1158/1535-7163.mct-17-1195.

<a href='https://doi.org/10.1021/acs.jnatprod.8b00432' target='_blank' class='bux-link'>Calothrixamides A and B from the Cultured Cyanobacterium Calothrix sp. UIC 10520</a>, Journal of Natural Products. 2018 Sep | journal-article. doi: 10.1021/acs.jnatprod.8b00432.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85043513125&partnerID=MN8TOARS' target='_blank' class='bux-link'>Incorporation of Selected Antimicrobial Small Molecule Compounds into Tapioca Starch and the Effects on Thickness, Moisture, and Oxygen Mass Transfer, and Mechanical Properties of the Films</a>, Starch/Staerke. 2018 Jan | journal-article. doi: 10.1002/star.201700060.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85045211790&partnerID=MN8TOARS' target='_blank' class='bux-link'>Synthesis and antiproliferative activity of derivatives of the phyllanthusmin class of arylnaphthalene lignan lactones</a>, Bioorganic and Medicinal Chemistry. 2018 Jan | journal-article. doi: 10.1016/j.bmc.2018.03.033.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85044420776&partnerID=MN8TOARS' target='_blank' class='bux-link'>Total Synthesis of Scytonemide A Employing Weinreb AM Solid-Phase Resin</a>, Journal of Natural Products. 2018 Jan | journal-article. doi: 10.1021/acs.jnatprod.7b00912.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85029808925&partnerID=MN8TOARS' target='_blank' class='bux-link'>Pentalinonsterol, a Constituent of Pentalinon andrieuxii, Possesses Potent Immunomodulatory Activity and Primes T Cell Immune Responses</a>, Journal of Natural Products. 2017 Jan | journal-article. doi: 10.1021/acs.jnatprod.7b00445.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-85036458337&partnerID=MN8TOARS' target='_blank' class='bux-link'>Resistance to pyridine-based inhibitor KF116 reveals an unexpected role of integrase in HIV-1 Gag-Pol polyprotein proteolytic processing</a>, Journal of Biological Chemistry. 2017 Jan | journal-article. doi: 10.1074/jbc.M117.816645.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84969248842&partnerID=MN8TOARS' target='_blank' class='bux-link'>A Novel Sterol Isolated from a Plant Used by Mayan Traditional Healers Is Effective in Treatment of Visceral Leishmaniasis Caused by Leishmania donovani</a>, ACS Infectious Diseases. 2016 Jan | journal-article. doi: 10.1021/acsinfecdis.5b00081.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84994257527&partnerID=MN8TOARS' target='_blank' class='bux-link'>A new class of allosteric HIV-1 integrase inhibitors identified by crystallographic fragment screening of the catalytic core domain</a>, Journal of Biological Chemistry. 2016 Jan | journal-article. doi: 10.1074/jbc.M116.753384.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84992371644&partnerID=MN8TOARS' target='_blank' class='bux-link'>Allosteric HIV-1 integrase inhibitors promote aberrant protein multimerization by directly mediating inter-subunit interactions: Structural and thermodynamic modeling studies</a>, Protein Science. 2016 Jan | journal-article. doi: 10.1002/pro.2997.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84982993414&partnerID=MN8TOARS' target='_blank' class='bux-link'>Computational and synthetic approaches for developing Lavendustin B derivatives as allosteric inhibitors of HIV-1 integrase</a>, European Journal of Medicinal Chemistry. 2016 Jan | journal-article. doi: 10.1016/j.ejmech.2016.07.077.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84993996126&partnerID=MN8TOARS' target='_blank' class='bux-link'>Discovery of anticancer agents of diverse natural origin</a>, Anticancer Research. 2016 Jan | journal-article. doi: 10.21873/anticanres.11146.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84983732388&partnerID=MN8TOARS' target='_blank' class='bux-link'>HIV-1 Integrase Binds the Viral RNA Genome and Is Essential during Virion Morphogenesis</a>, Cell. 2016 Jan | journal-article. doi: 10.1016/j.cell.2016.07.044.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84985942541&partnerID=MN8TOARS' target='_blank' class='bux-link'>Indole-based allosteric inhibitors of HIV-1 integrase</a>, Bioorganic and Medicinal Chemistry Letters. 2016 Jan | journal-article. doi: 10.1016/j.bmcl.2016.08.037.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84959181076&partnerID=MN8TOARS' target='_blank' class='bux-link'>Insertional Mutagenesis Identifies a STAT3/Arid1b/β-catenin Pathway Driving Neurofibroma Initiation</a>, Cell Reports. 2016 Jan | journal-article. doi: 10.1016/j.celrep.2016.01.074.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84966359102&partnerID=MN8TOARS' target='_blank' class='bux-link'>Novel anti-campylobacter compounds identified using high throughput screening of a pre-selected enriched small molecules library</a>, Frontiers in Microbiology. 2016 Jan | journal-article. doi: 10.3389/fmicb.2016.00405.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84962018821&partnerID=MN8TOARS' target='_blank' class='bux-link'>Overcoming chemo/radio-resistance of pancreatic cancer by inhibiting STAT3 signaling</a>, Oncotarget. 2016 Jan | journal-article. doi: 10.18632/oncotarget.7336.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84955242357&partnerID=MN8TOARS' target='_blank' class='bux-link'>Preclinical in vitro, in vivo, and pharmacokinetic evaluations of FLLL12 for the prevention and treatment of head and neck cancers</a>, Cancer Prevention Research. 2016 Jan | journal-article. doi: 10.1158/1940-6207.CAPR-15-0240.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84996536976&partnerID=MN8TOARS' target='_blank' class='bux-link'>STAT3 as a potential therapeutic target in ALDH+ and CD44+/CD24+stem cell-like pancreatic cancer cells</a>, International Journal of Oncology. 2016 Jan | journal-article. doi: 10.3892/ijo.2016.3728.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84971310272&partnerID=MN8TOARS' target='_blank' class='bux-link'>The Competitive Interplay between Allosteric HIV-1 Integrase Inhibitor BI/D and LEDGF/p75 during the Early Stage of HIV-1 Replication Adversely Affects Inhibitor Potency</a>, ACS Chemical Biology. 2016 Jan | journal-article. doi: 10.1021/acschembio.6b00167.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84922728730&partnerID=MN8TOARS' target='_blank' class='bux-link'>Cytotoxic and natural killer cell stimulatory constituents of Phyllanthus songboiensis</a>, Phytochemistry. 2015 Jan | journal-article. doi: 10.1016/j.phytochem.2014.12.014.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84946831515&partnerID=MN8TOARS' target='_blank' class='bux-link'>Discovery of novel small molecule modulators of Clavibacter michiganensis subsp. michiganensis</a>, Frontiers in Microbiology. 2015 Jan | journal-article. doi: 10.3389/fmicb.2015.01127.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84940994512&partnerID=MN8TOARS' target='_blank' class='bux-link'>Distribution and redistribution of HIV-1 nucleocapsid protein in immature, mature, and integrase-inhibited virions: A role for integrase in maturation</a>, Journal of Virology. 2015 Jan | journal-article. doi: 10.1128/JVI.01522-15.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84929282397&partnerID=MN8TOARS' target='_blank' class='bux-link'>FLLL12 induces apoptosis in lung cancer cells through a p53/p73-independent but death receptor 5-dependent pathway</a>, Cancer Letters. 2015 Jan | journal-article. doi: 10.1016/j.canlet.2015.04.017.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84926643036&partnerID=MN8TOARS' target='_blank' class='bux-link'>Inhibition of the JAK2/STAT3 signaling pathway exerts a therapeutic effect on osteosarcoma</a>, Molecular Medicine Reports. 2015 Jan | journal-article. doi: 10.3892/mmr.2015.3439.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84937404051&partnerID=MN8TOARS' target='_blank' class='bux-link'>Trichormamides C and D, antiproliferative cyclic lipopeptides from the cultured freshwater cyanobacterium cf. Oscillatoria sp. UIC 10045</a>, Bioorganic and Medicinal Chemistry. 2015 Jan | journal-article. doi: 10.1016/j.bmc.2015.04.073.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84901657154&partnerID=MN8TOARS' target='_blank' class='bux-link'>A New Class of Multimerization Selective Inhibitors of HIV-1 Integrase</a>, PLoS Pathogens. 2014 Jan | journal-article. doi: 10.1371/journal.ppat.1004171.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84907222847&partnerID=MN8TOARS' target='_blank' class='bux-link'>A critical role of the C-terminal segment for allosteric inhibitor-induced aberrant multimerization of HIV-1 integrase</a>, Journal of Biological Chemistry. 2014 Jan | journal-article. doi: 10.1074/jbc.M114.589572.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84891940023&partnerID=MN8TOARS' target='_blank' class='bux-link'>EGFR-STAT3 signaling promotes formation of malignant peripheral nerve sheath tumors</a>, Oncogene. 2014 Jan | journal-article. doi: 10.1038/onc.2012.579.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84903639618&partnerID=MN8TOARS' target='_blank' class='bux-link'>Potent cytotoxic arylnaphthalene lignan lactones from Phyllanthus poilanei</a>, Journal of Natural Products. 2014 Jan | journal-article. doi: 10.1021/np5002785.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84902295879&partnerID=MN8TOARS' target='_blank' class='bux-link'>Rocaglamide, silvestrol and structurally related bioactive compounds from Aglaia species</a>, Natural Product Reports. 2014 Jan | journal-article. doi: 10.1039/c4np00006d.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84907224797&partnerID=MN8TOARS' target='_blank' class='bux-link'>TALEN knockout of the PSIP1 gene in human cells: Analyses of HIV-1 replication and allosteric integrase inhibitor mechanism</a>, Journal of Virology. 2014 Jan | journal-article. doi: 10.1128/JVI.01397-14.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84934915505&partnerID=MN8TOARS' target='_blank' class='bux-link'>The mechanism of H171T resistance reveals the importance of N<inf>δ</inf>-protonated His171 for the binding of allosteric inhibitor BI-D to HIV-1 integrase</a>, Retrovirology. 2014 Jan | journal-article. doi: 10.1186/s12977-014-0100-1.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84906708303&partnerID=MN8TOARS' target='_blank' class='bux-link'>Trichormamides A and B with antiproliferative activity from the cultured freshwater cyanobacterium Trichormus sp. UIC 10339</a>, Journal of Natural Products. 2014 Jan | journal-article. doi: 10.1021/np5003548.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84878137599&partnerID=MN8TOARS' target='_blank' class='bux-link'>Allosteric integrase inhibitor potency is determined through the inhibition of HIV-1 particle maturation</a>, Proceedings of the National Academy of Sciences of the United States of America. 2013 Jan | journal-article. doi: 10.1073/pnas.1300703110.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84875425408&partnerID=MN8TOARS' target='_blank' class='bux-link'>Bioactive flavaglines and other constituents isolated from Aglaia perviridis</a>, Journal of Natural Products. 2013 Jan | journal-article. doi: 10.1021/np3007588.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84890597865&partnerID=MN8TOARS' target='_blank' class='bux-link'>HAb18G/CD147 promotes pSTAT3-mediated pancreatic cancer development via CD44s</a>, Clinical Cancer Research. 2013 Jan | journal-article. doi: 10.1158/1078-0432.CCR-13-0621.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84877848590&partnerID=MN8TOARS' target='_blank' class='bux-link'>Pancreatic cancer-associated stellate cells promote differentiation of myeloid-derived suppressor cells in a StAT3-dependent manner</a>, Cancer Research. 2013 Jan | journal-article. doi: 10.1158/0008-5472.CAN-12-4601.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84878408619&partnerID=MN8TOARS' target='_blank' class='bux-link'>The A128T resistance mutation reveals aberrant protein multimerization as the primary mechanism of action of allosteric HIV-1 integrase inhibitors</a>, Journal of Biological Chemistry. 2013 Jan | journal-article. doi: 10.1074/jbc.M112.443390.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84871220094&partnerID=MN8TOARS' target='_blank' class='bux-link'>HRP2 determines the efficiency and specificity of HIV-1 integration in LEDGF/p75 knockout cells but does not contribute to the antiviral activity of a potent LEDGF/p75-binding site integrase inhibitor</a>, Nucleic Acids Research. 2012 Jan | journal-article. doi: 10.1093/nar/gks913.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84860871902&partnerID=MN8TOARS' target='_blank' class='bux-link'>Multimode, cooperative mechanism of action of allosteric HIV-1 integrase inhibitors</a>, Journal of Biological Chemistry. 2012 Jan | journal-article. doi: 10.1074/jbc.M112.354373.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84865268573&partnerID=MN8TOARS' target='_blank' class='bux-link'>Sterols with antileishmanial activity isolated from the roots of Pentalinon andrieuxii</a>, Phytochemistry. 2012 Jan | journal-article. doi: 10.1016/j.phytochem.2012.06.012.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84934439853&partnerID=MN8TOARS' target='_blank' class='bux-link'>Use of the hollow fiber assay for the discovery of novel anticancer agents from fungi</a>, Methods in Molecular Biology. 2012 Jan | book. doi: 10.1007/978-1-62703-122-6_20.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-79957802468&partnerID=MN8TOARS' target='_blank' class='bux-link'>Cytotoxic and NF-κB inhibitory constituents of the stems of Cratoxylum cochinchinense and their semisynthetic analogues</a>, Journal of Natural Products. 2011 Jan | journal-article. doi: 10.1021/np200051j.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-84855876635&partnerID=MN8TOARS' target='_blank' class='bux-link'>STAT3 signaling pathway is necessary for cell survival and tumorsphere forming capacity in ALDH+/CD133+stem cell-like human colon cancer cells</a>, Biochemical and Biophysical Research Communications. 2011 Jan | journal-article. doi: 10.1016/j.bbrc.2011.10.112.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-79956140623&partnerID=MN8TOARS' target='_blank' class='bux-link'>Sensitization of head and neck cancer to cisplatin through the use of a novel curcumin analog</a>, Archives of Otolaryngology - Head and Neck Surgery. 2011 Jan | journal-article. doi: 10.1001/archoto.2011.63.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-78049483745&partnerID=MN8TOARS' target='_blank' class='bux-link'>A liquid chromatography-tandem mass spectrometric method for quantification of curcuminoids in cell medium and mouse plasma</a>, Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences. 2010 Jan | journal-article. doi: 10.1016/j.jchromb.2010.08.039.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-77956409919&partnerID=MN8TOARS' target='_blank' class='bux-link'>IL-6, a risk factor for hepatocellular carcinoma: FLLL32 inhibits IL-6-induced STAT3 phosphorylation in human hepatocellular cancer cells</a>, Cell Cycle. 2010 Jan | journal-article. doi: 10.4161/cc.9.17.12946.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-70349479218&partnerID=MN8TOARS' target='_blank' class='bux-link'>Curcumin induces proapoptotic effects against human melanoma cells and modulates the cellular response to immunotherapeutic cytokines</a>, Molecular Cancer Therapeutics. 2009 Jan | journal-article. doi: 10.1158/1535-7163.MCT-09-0377.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-33747610224&partnerID=MN8TOARS' target='_blank' class='bux-link'>Intramolecular diels-alder/1,3-dipolar cycloaddition cascade of 1,3,4-oxadiazoles</a>, Journal of the American Chemical Society. 2006 Jan | journal-article. doi: 10.1021/ja0612549.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-14844363196&partnerID=MN8TOARS' target='_blank' class='bux-link'>Indol-2-one intermediates: Mechanistic evidence and synthetic utility. Total syntheses of (±)-flustramines A and C</a>, Organic Letters. 2005 Jan | journal-article. doi: 10.1021/ol047532v.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-1942489302&partnerID=MN8TOARS' target='_blank' class='bux-link'>Total Synthesis of (±)-Perophoramidine</a>, Journal of the American Chemical Society. 2004 Jan | journal-article. doi: 10.1021/ja049569g.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0035909641&partnerID=MN8TOARS' target='_blank' class='bux-link'>Intramolecular electrophilic aromatic substitution reactions of 2-amidoacroleins: A new method for the preparation of tetrahydroisoquinolines, tetrahydro-3-benzazepines, and hexahydro-3-benzazocines</a>, Organic Letters. 2001 Jan | journal-article. doi: 10.1021/ol016592n.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0035969615&partnerID=MN8TOARS' target='_blank' class='bux-link'>Total synthesis of (±)-lennoxamine and (±)-aphanorphine by intramolecular electrophilic aromatic substitution reactions of 2-amidoacroleins</a>, Organic Letters. 2001 Jan | journal-article. doi: 10.1021/ol016795b.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0034674964&partnerID=MN8TOARS' target='_blank' class='bux-link'>Reactions of SmI<inf>2</inf>with alkyl halides and ketones: Inner-sphere vs outer-sphere electron transfer in reactions of Sm(II) reductants</a>, Journal of the American Chemical Society. 2000 Jan | journal-article. doi: 10.1021/ja001260j.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0032543505&partnerID=MN8TOARS' target='_blank' class='bux-link'>The effect of cosolvent on the reducing power of SmI<inf>2</inf>in tetrahydrofuran</a>, Tetrahedron Letters. 1998 Jan | journal-article. doi: 10.1016/S0040-4039(98)00839-9.

<a href='http://www.scopus.com/inward/record.url?eid=2-s2.0-0030683498&partnerID=MN8TOARS' target='_blank' class='bux-link'>The effect of lithium bromide and lithium chloride on the reactivity of SmI<inf>2</inf>in THF</a>, Tetrahedron Letters. 1997 Jan | journal-article. doi: 10.1016/S0040-4039(97)10222-2.

Xiaolin Cheng

Professor

Medicinal Chemistry and Pharmacognosy

Research Areas

Cancer,

Infectious Diseases,

Chemical Biology,

Computational Biomedicine & Data Analytics,

Medicinal Chemistry & Pharmacognosy

5041 Pelotonia Research Center

cheng.1302@osu.edu

(614) 292-3198

Professional Website

Dr. Cheng’s laboratory aims to develop an interdisciplinary research program centered on Computer Aided Drug Design and Discovery. Closely collaborating with experimental chemists and biologists, our group utilizes a myriad of computational modeling & simulation, and data analytics techniques to understand molecular basis of drug action and to rationally design new drug molecules. Our group also has long-standing interests in: a) developing and applying multiscale computational techniques to investigate the structure, dynamics and function of complex biomolecular (and cellular ) systems; and b) bridge large-scale molecular simulation with systems biology (cellular metabolism and signaling networks) towards a new drug discovery paradigm.

Kong X, Xing E, Zhuang T, Li PK, Cheng X. Mechanistic Insights into the Allosteric Inhibition of Androgen Receptors by Binding Function 3 Antagonists from an Integrated Molecular Modeling Study. J Chem Inf Model. 2021 Jun 24. doi: 10.1021/acs.jcim.1c00124. Epub ahead of print. PMID: 34165949.

Ren Y, Wu S, Burdette JE, Cheng X, Kinghorn AD. Structural Insights into the Interactions of Digoxin and Na+/K+-ATPase and Other Targets for the Inhibition of Cancer Cell Proliferation. Molecules. 2021 Jun 16;26(12):3672. doi: 10.3390/molecules26123672. PMID: 34208576; PMCID: PMC8234910.

Farago B, Nicholl ID, Wang S, Cheng X, Callaway DJE, Bu Z. Activated nanoscale actin-binding domain motion in the catenin-cadherin complex revealed by neutron spin echo spectroscopy. Proc Natl Acad Sci U S A. 2021 Mar 30;118(13):e2025012118. doi: 10.1073/pnas.2025012118. PMID: 33753508; PMCID: PMC8020631.

Saeed AFUH, Chan C, Guan H, Gong B, Guo P, Cheng X, Ouyang S. Structural Insights into gp16 ATPase in the Bacteriophage ϕ29 DNA Packaging Motor. Biochemistry. 2021 Mar 23;60(11):886-897. doi: 10.1021/acs.biochem.0c00935. Epub 2021 Mar 9. PMID: 33689296.

Li T, Kong L, Li X, Wu S, Attri KS, Li Y, Gong W, Zhao B, Li L, Herring LE, Asara JM, Xu L, Luo X, Lei YL, Ma Q, Seveau S, Gunn JS, Cheng X, Singh PK, Green DR, Wang H, Wen H. Listeria monocytogenes upregulates mitochondrial calcium signalling to inhibit LC3-associated phagocytosis as a survival strategy. Nat Microbiol. 2021 Mar;6(3):366-379. doi: 10.1038/s41564-020-00843-2. Epub 2021 Jan 18. PMID: 33462436.

Persaud AK, Nair S, Rahman MF, Raj R, Weadick B, Nayak D, McElroy C, Shanmugam M, Knoblaugh S, Cheng X, Govindarajan R. Facilitative lysosomal transport of bile acids alleviates ER stress in mouse hematopoietic precursors. Nat Commun. 2021 Feb 23;12(1):1248. doi: 10.1038/s41467-021-21451-6. PMID: 33623001; PMCID: PMC7902824.

Chan C, Du S, Dong Y, Cheng X. Computational and Experimental Approaches to Investigate Lipid Nanoparticles as Drug and Gene Delivery Systems. Curr Top Med Chem. 2021;21(2):92-114. doi: 10.2174/1568026620666201126162945. PMID: 33243123; PMCID: PMC8191596.

Wu S, Chan C, Zhuang T, Li PK, Cheng X. A computational study of effects on membrane recruitment of the polar linkers in Vitamin E derivatives. Biochim Biophys Acta Gen Subj. 2020 Oct;1864(10):129655. doi: 10.1016/j.bbagen.2020.129655. Epub 2020 Jun 11. PMID: 32535151.

Marquardt D, Heberle FA, Pan J, Cheng X, Pabst G, Harroun TA, Kučerka N, Katsaras J. The structures of polyunsaturated lipid bilayers by joint refinement of neutron and X-ray scattering data. Chem Phys Lipids. 2020 Jul;229:104892. doi: 10.1016/j.chemphyslip.2020.104892. Epub 2020 Feb 12. PMID: 32061581.

Liu E, Zhang ZZ, Cheng X, Liu X, Cheng L. SCNrank: spectral clustering for network-based ranking to reveal potential drug targets and its application in pancreatic ductal adenocarcinoma. BMC Med Genomics. 2020 Apr 3;13(Suppl 5):50. doi: 10.1186/s12920-020-0681-6. PMID: 32241274; PMCID: PMC7119297.

Gorecki L, Gerlits O, Kong X, Cheng X, Blumenthal DK, Taylor P, Ballatore C, Kovalevsky A, Radić Z. Rational design, synthesis, and evaluation of uncharged, "smart" bis-oxime antidotes of organophosphate-inhibited human acetylcholinesterase. J Biol Chem. 2020 Mar 27;295(13):4079-4092. doi: 10.1074/jbc.RA119.012400. Epub 2020 Feb 4. Erratum in: J Biol Chem. 2020 May 8;295(19):6784. PMID: 32019865; PMCID: PMC7105318.

Ren Y, Ribas HT, Heath K, Wu S, Ren J, Shriwas P, Chen X, Johnson ME, Cheng X, Burdette JE, Kinghorn AD. Na+/K+-ATPase-Targeted Cytotoxicity of (+)-Digoxin and Several Semisynthetic Derivatives. J Nat Prod. 2020 Mar 27;83(3):638-648. doi: 10.1021/acs.jnatprod.9b01060. Epub 2020 Feb 25. PMID: 32096998; PMCID: PMC7243443.

Li W, Chan C, Zeng C, Turk R, Behlke MA, Cheng X, Dong Y. Rational Design of Small Molecules to Enhance Genome Editing Efficiency by Selectively Targeting Distinct Functional States of CRISPR-Cas12a. Bioconjug Chem. 2020 Mar 18;31(3):542-546. doi: 10.1021/acs.bioconjchem.0c00062. Epub 2020 Mar 6. PMID: 32119776; PMCID: PMC8192075.

Manwill PK, Kalsi M, Wu S, Martinez Rodriguez EJ, Cheng X, Piermarini PM, Rakotondraibe HL. Semi-synthetic cinnamodial analogues: Structural insights into the insecticidal and antifeedant activities of drimane sesquiterpenes against the mosquito Aedes aegypti. PLoS Negl Trop Dis. 2020 Feb 26;14(2):e0008073. doi: 10.1371/journal.pntd.0008073. PMID: 32101555; PMCID: PMC7062286.

Ren Y, Tan Q, Heath K, Wu S, Wilson JR, Ren J, Shriwas P, Yuan C, Ngoc Ninh T, Chai HB, Chen X, Soejarto DD, Johnson ME, Cheng X, Burdette JE, Kinghorn AD. Cytotoxic and non-cytotoxic cardiac glycosides isolated from the combined flowers, leaves, and twigs of Streblus asper. Bioorg Med Chem. 2020 Feb 15;28(4):115301. doi: 10.1016/j.bmc.2019.115301. Epub 2020 Jan 7. PMID: 31953129; PMCID: PMC7029422.

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