Bob Brueggemeier

Robert Brueggemeier

Bob Brueggemeier, PhD

Faculty Emeritus
brueggemeier.1@osu.edu
(614) 292-5231

Education

  • 1977, PhD, University of Michigan, Medicinal Chemistry
  • 1975, MS, University of Michigan, Medicinal Chemistry
  • 1972, BA, Michigan State University, Chemistry

Honors

  • Outstanding Dean Award, 2011 - 2011
  • Tyler Prize for Stimulation of Research Award, 2008
  • AAAS Fellow, 1999
  • AAPS Fellow, 1997

Publications

  • Su, Bin; Mershon, Serena M.; Stonerock, Laura A.; Curley, Robert W., Jr.; Brueggemeier, Robert W. 4-hydroxyphenylretinamide (4hpr) derivatives regulate aromatase activity and expression in breast cancer cells Journal of Steroid Biochemistry and Molecular Biology. 2008 Jan; 109(1-2):40-46.
  • Davis, Danyetta D.; Diaz-Cruz, Edgar S.; Landini, Serena; Kim, Young-Woo; Brueggemeier, Robert W. Evaluation of synthetic isoflavones on cell proliferation, estrogen receptor binding affinity, and apoptosis in human breast cancer cells Journal of Steroid Biochemistry and Molecular Biology. 2008 Jan; 108(1-2):23-31.
  • Su, Bin; Landini, Serena; Davis, Danyetta, D; Brueggemeier, Robert W Synthesis and biological evaluation of selective aromatase expression regulators in breast cancer cells. Journal of medicinal chemistry. 2007 Jan; 50(7):1635-44.
  • Hackett, John; Xiao, Zili; Zang, Xiao-Ping; Lerner, Megan L.; Brackett, Daniel J.; Brueggemeier, Robert W.; Li, Pui-Kai; Pento, J. Thomas Development of keratinocyte growth factor receptor tyrosine kinase inhibitors for the treatment of cancer Anticancer Research. 2007 Jan; 27(6B):3801-3806.
  • Hackett, John; Xiao, Zili; Zang, Xiao-Ping; Lerner, Megan, L; Brackett, Daniel, J; Brueggemeier, Robert, W; Li, Pui-Kai; Pento, J Thomas Development of keratinocyte growth factor receptor tyrosine kinase inhibitors for the treatment of cancer. Anticancer research. 2007 Jan; 27(6B):.
  • Brueggemeier, Robert, W; Su, Bin; Sugimoto, Yasuro; Diaz-Cruz, Edgar, S; Davis, Danyetta D Aromatase and COX in breast cancer: enzyme inhibitors and beyond. The Journal of steroid biochemistry and molecular biology. 2007 Jan; 106(1-5):.
  • Su, Bin; Diaz-Cruz, Edgar, S; Landini, Serena; Brueggemeier, Robert W Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition. Journal of medicinal chemistry. 2006 Jan; 49(4):1413-9.
  • Diaz-Cruz, Edgar, S; Brueggemeier, Robert W Interrelationships between cyclooxygenases and aromatase: unraveling the relevance of cyclooxygenase inhibitors in breast cancer. Anticancer Agents Med Chem. 2006 Jan; 6(3):221-32.
  • Brueggemeier, Robert W Update on the use of aromatase inhibitors in breast cancer. Expert opinion on pharmacotherapy. 2006 Jan; 7(14):1919-30.
  • Tseng, Ping-Hui; Wang, Yu-Chieh; Weng, Shu-Chuan; Weng, Jing-Ru; Chen, Chang-Shi; Brueggemeier, Robert, W; Shapiro, Charles, L; Chen, Ching-Yu; Dunn, Sandra, E; Pollak, Michael; Chen, Ching-Shih Overcoming trastuzumab resistance in HER2-overexpressing breast cancer cells by using a novel celecoxib-derived phosphoinositide-dependent kinase-1 inhibitor. Molecular pharmacology. 2006 Jan; 70(5):1534-41.
  • Brueggemeier, R, W; Diaz-Cruz, E S Relationship between aromatase and cyclooxygenases in breast cancer: potential for new therapeutic approaches. Minerva endocrinologica. 2006 Jan; 31(1):13-26.
  • Brueggemeier, Robert, W; Diaz-Cruz, Edgar, S; Li, Pui-Kai; Sugimoto, Yasuro; Lin, Young, C; Shapiro, Charles L Translational studies on aromatase, cyclooxygenases, and enzyme inhibitors in breast cancer. The Journal of steroid biochemistry and molecular biology. 2005 Jan; 95(1-5):129-36.
  • Huang, Jui-Wen; Shiau, Chung-Wai; Yang, Ya-Ting; Kulp, Samuel, K; Chen, Kuen-Feng; Brueggemeier, Robert, W; Shapiro, Charles, L; Chen, Ching-Shih Peroxisome proliferator-activated receptor gamma-independent ablation of cyclin D1 by thiazolidinediones and their derivatives in breast cancer cells. Molecular pharmacology. 2005 Jan; 67(4):1342-8.
  • Diaz-Cruz, Edgar, S; Shapiro, Charles, L; Brueggemeier, Robert W Cyclooxygenase inhibitors suppress aromatase expression and activity in breast cancer cells. The Journal of clinical endocrinology and metabolism. 2005 Jan; 90(5):2563-70.
  • Brueggemeier, Robert W Aromatase inhibitors: new endocrine treatment of breast cancer. Seminars in reproductive medicine. 2004 Jan; 22(1):31-43.
  • Mobley, James, A; Brueggemeier, Robert W Estrogen receptor-mediated regulation of oxidative stress and DNA damage in breast cancer. Carcinogenesis. 2004 Jan; 25(1):3-9.
  • Kim, Young-Woo; Mobley, James, A; Brueggemeier, Robert W Synthesis and estrogen receptor binding affinities of 7-hydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-ones containing a basic side chain. Bioorganic & medicinal chemistry letters. 2003 Jan; 13(8):1475-8.
  • Petrel, Trevor, A; Brueggemeier, Robert W Increased proteasome-dependent degradation of estrogen receptor-alpha by TGF-beta1 in breast cancer cell lines. Journal of cellular biochemistry. 2003 Jan; 88(1):181-90.
  • Mobley, James, A; Brueggemeier, Robert W Increasing the DNA damage threshold in breast cancer cells. Toxicology and applied pharmacology. 2002 Jan; 180(3):219-26.
  • Brueggemeier, Robert W Aromatase inhibitors in breast cancer therapy. Expert review of anticancer therapy. 2002 Jan; 2(2):181-91.
  • Brueggemeier, Robert W Overview of the pharmacology of the aromatase inactivator exemestane. Breast cancer research and treatment. 2002 Jan; 74(2):177-85.
  • Brueggemeier, R W Aromatase, aromatase inhibitors, and breast cancer. American journal of therapeutics. 2001 Jan; 8(5):333-44.
  • Brueggemeier, R, W; Bhat, A, S; Lovely, C, J; Coughenour, H, D; Joomprabutra, S; Weitzel, D, H; Vandre, D, D; Yusuf, F; Burak, W E Jr 2-Methoxymethylestradiol: a new 2-methoxy estrogen analog that exhibits antiproliferative activity and alters tubulin dynamics. The Journal of steroid biochemistry and molecular biology. 2001 Jan; 78(2):145-56.
  • Lynch, M, A; Petrel, T, A; Song, H; Knobloch, T, J; Casto, B, C; Ramljak, D; Anderson, L, M; DeGroff, V; Stoner, G, D; Brueggemeier, R, W; Weghorst, C M Responsiveness to transforming growth factor-beta (TGF-beta)-mediated growth inhibition is a function of membrane-bound TGF-beta type II receptor in human breast cancer cells. Gene expression. 2001 Jan; 9(4-5):157-71.
  • Zheng, J; Kulp, S, K; Zhang, Y; Sugimoto, Y; Dayton, M, A; Govindan, M, V; Brueggemeier, R, W; Lin, Y C 17 beta-estradiol-regulated expression of protein tyrosine phosphatase gamma gene in cultured human normal breast and breast cancer cells. Anticancer research. 2000 Jan; 20(1A):11-9.
  • Mobley, J, A; Bhat, A, S; Brueggemeier, R W Measurement of oxidative DNA damage by catechol estrogens and analogues in vitro. Chemical research in toxicology. 1999 Jan; 12(3):270-7.
  • Harris, R, E; Robertson, F, M; Abou-Issa, H, M; Farrar, W, B; Brueggemeier, R Genetic induction and upregulation of cyclooxygenase (COX) and aromatase (CYP19): an extension of the dietary fat hypothesis of breast cancer. Medical hypotheses. 1999 Jan; 52(4):291-2.
  • Quinn, A, L; Burak, W E Jr; Brueggemeier, R W Effects of matrix components on aromatase activity in breast stromal cells in culture. The Journal of steroid biochemistry and molecular biology. 1999 Jan; 70(4-6):249-56.
  • Brueggemeier, R, W; Quinn, A, L; Parrett, M, L; Joarder, F, S; Harris, R, E; Robertson, F M Correlation of aromatase and cyclooxygenase gene expression in human breast cancer specimens. Cancer letters. 1999 Jan; 140(1-2):27-35.
  • Zhang, Y; Kulp, S, K; Sugimoto, Y; Farrar, W, B; Brueggemeier, R, W; Lin, Y C Keratinocyte growth factor (KGF) induces aromatase activity in cultured MCF-7 human breast cancer cells. Anticancer research. 1998 Jan; 18(4A):2541-6.
  • Zhang, Y; Kulp, S, K; Sugimoto, Y; Brueggemeier, R, W; Lin, Y C The (-)-enantiomer of gossypol inhibits proliferation of stromal cells derived from human breast adipose tissues by enhancing transforming growth factor beta1 production. International journal of oncology. 1998 Jan; 13(6):1291-7.
  • Zhang, Y; Sugimoto, Y; Kulp, S, K; Farrar, W, B; Brueggemeier, R, W; Lin, Y C Estrogen-induced keratinocyte growth factor mRNA expression in normal and cancerous human breast cells. Oncology reports. 1998 Jan; 5(3):577-83.
  • Lovely, C, J; Bhat, A, S; Coughenour, H, D; Gilbert, N, E; Brueggemeier, R W Synthesis and biological evaluation of 4-(hydroxyalkyl)estradiols and related compounds. Journal of medicinal chemistry. 1997 Jan; 40(23):3756-64.
  • Burak, W E Jr; Quinn, A, L; Farrar, W, B; Brueggemeier, R W Androgens influence estrogen-induced responses in human breast carcinoma cells through cytochrome P450 aromatase. Breast cancer research and treatment. 1997 Jan; 44(1):57-64.
  • Brueggemeier, R, W; Gilbert, N, E; Gu, ; XO'Reilly, J, M; Lovely, C J Aromatase inhibition in JAr choriocarcinoma cells by 7alpha-arylaliphatic androgens. The Journal of steroid biochemistry and molecular biology. 1997 Jan; 61(1-2):73-7.
  • Shidaifat, F; Canatan, H; Kulp, S, K; Sugimoto, Y; Zhang, Y; Brueggemeier, R, W; Somers, W, J; Chang, W, Y; Wang, H, C; Lin, Y C Gossypol arrests human benign prostatic hyperplastic cell growth at G0/G1 phase of the cell cycle. Anticancer research. 1997 Jan; 17(2A):1003-9.
  • Shidaifat, F; Canatan, H; Kulp, S, K; Sugimoto, Y; Chang, W, Y; Zhang, Y; Brueggemeier, R, W; Somers, W, J; Lin, Y C Inhibition of human prostate cancer cells growth by gossypol is associated with stimulation of transforming growth factor-beta. Cancer letters. 1996 Jan; 107(1):37-44.
  • O'Reilly, Jill M.; Brueggemeier, Robert W. 7-alpha-arylaliphatic Androsta-1,4-diene-3,17-diones as enzyme-activated irreversible inhibitors of aromatase Journal of Steroid Biochemistry and Molecular Biology. 1996 Jan; 59(1):93-102.
  • Chang, W, Y; Shidaifat, F; Chang, C, J; Kulp, S, K; Sugimoto, Y; Canatan, H; Brueggemeier, R, W; Lin, Y C Experimentally-induced prostatic hyperplasia in young beagles: a model to evaluate the chemotherapeutic effects of gossypol. Research communications in molecular pathology and pharmacology. 1996 Jan; 92(3):341-60.
  • Lovely, C, J; Gilbert, N, E; Liberto, M, M; Sharp, D, W; Lin, Y, C; Brueggemeier, R W 2-(Hydroxyalkyl)estradiols: synthesis and biological evaluation. Journal of medicinal chemistry. 1996 Jan; 39(9):1917-23.
  • Canatan, H; Chang, W, Y; Sugimoto, Y; Shidaifat, F; Kulp, S, K; Brueggemeier, R, W; Lin, Y C Keratinocyte growth factor (KGF/FGF-7) has a paracrine role in canine prostate: molecular cloning of mRNA encoding canine KGF. DNA and cell biology. 1996 Jan; 15(3):247-54.
  • O'Reilly, J, M; Brueggemeier, R W 7alpha-Arylaliphatic androsta-1,4-diene-3,17-diones as enzyme-activated irreversible inhibitors of aromatase. The Journal of steroid biochemistry and molecular biology. 1996 Jan; 59(1):93-102.
  • Gilbert, N, E; O'Reilly, J, E; Chang, C, J; Lin, Y, C; Brueggemeier, R W Antiproliferative activity of gossypol and gossypolone on human breast cancer cells. Life sciences. 1995 Jan; 57(1):61-7.
  • Beleh, M, A; Lin, Y, C; Brueggemeier, R W Estrogen metabolism in microsomal, cell, and tissue preparations of kidney and liver from Syrian hamsters. The Journal of steroid biochemistry and molecular biology. 1995 Jan; 52(5):479-89.
  • O'Reilly, J, M; Li, N; Duax, W, L; Brueggemeier, R W Synthesis, structure elucidation, and biochemical evaluation of 7 alpha- and 7 beta-arylaliphatic-substituted androst-4-ene-3,17-diones as inhibitors of aromatase. Journal of medicinal chemistry. 1995 Jan; 38(15):2842-50.
  • Lin, Y, C; Canatan, H; Chang, C, J; Hu, Y, F; Chen, R; Yu, C, Y; Brueggemeier, R, W; Somers, W J Detection of keratinocyte growth factor (KGF) transcripts from normal human and archival canine benign prostatic hyperplastic tissues. Journal of medicine. 1994 Jan; 25(1-2):41-64.
  • Brueggemeier, R W Aromatase inhibitors--mechanisms of steroidal inhibitors. Breast cancer research and treatment. 1994 Jan; 30(1):31-42.
  • Hu, Y, F; Chang, C, J; Brueggemeier, R, W; Lin, Y C Presence of antitumor activities in the milk collected from gossypol-treated dairy cows. Cancer letters. 1994 Jan; 87(1):17-23.
  • Beleh, M, A; Brueggemeier, R, W; Chang, G, C; Lin, Y C Biosynthesis and secretion of growth factor proteins by kidney cells from DES-treated Syrian hamsters. Biochemical and biophysical research communications. 1993 Jan; 190(3):1029-36.
  • Hu, Y, F; Chang, C, J; Brueggemeier, R, W; Lin, Y C Gossypol inhibits basal and estrogen-stimulated DNA synthesis in human breast carcinoma cells. Life sciences. 1993 Jan; 53(25):PL433-8.
  • Moh, P, P; Chang, G, C; Brueggemeier, R, W; Lin, Y C Effect of gossypol on 5 alpha-reductase and 3 alpha-hydroxysteroid dehydrogenase activities in adult rat testes. Research communications in chemical pathology and pharmacology. 1993 Jan; 82(1):12-26.
  • Chang, C, J; Ghosh, P, K; Hu, Y, F; Brueggemeier, R, W; Lin, Y C Antiproliferative and antimetastatic effects of gossypol on Dunning prostate cell-bearing Copenhagen rats. Research communications in chemical pathology and pharmacology. 1993 Jan; 79(3):293-312.
  • Ebrahimian, S; Chen, H, H; Brueggemeier, R W Synthesis and biochemical studies of 7 alpha-substituted androsta-1,4-diene-3,17-diones as enzyme-activated irreversible inhibitors of aromatase. Steroids. 1993 Jan; 58(9):414-22.
  • Lin, Y, C; Gu, Y; Brueggemeier, R, W; Rikihisa, Y Binding of 3H-gossypol in organelles of cultured bovine luteal cells. Life sciences. 1992 Jan; 50(6):443-7.
  • Chang, C, J; Lin, Y, C; Brueggemeier, R, W; Rikihisa, Y Morphometric analysis of renal cortex changes induced by diethylstilbestrol (DES) in Syrian hamsters. Research communications in chemical pathology and pharmacology. 1992 Jan; 78(3):341-58.
  • Brueggemeier, R, W; Katlic, N, E; Kenreigh, C, A; Li, P K Aromatase inhibition by 7-substituted steroids in human choriocarcinoma cell culture. The Journal of steroid biochemistry and molecular biology. 1992 Jan; 41(1):85-90.
  • Gu, Y; Li, P, K; Lin, Y, C; Rikihisa, Y; Brueggemeier, R W Gossypolone suppresses progesterone synthesis in bovine luteal cells. The Journal of steroid biochemistry and molecular biology. 1991 Jan; 38(6):709-15.
  • Li, P, K; Brueggemeier, R W 7-substituted steroidal aromatase inhibitors: structure-activity relationships and molecular modeling. Journal of enzyme inhibition. 1990 Jan; 4(2):113-20.
  • Li, P, K; Brueggemeier, R W 7-substituted 1,4,6-androstatriene-3,17-diones as enzyme-activated irreversible inhibitors of aromatase. Journal of steroid biochemistry. 1990 Jan; 36(6):533-9.
  • Brueggemeier, R, W; Tseng, K; Katlic, N, E; Beleh, M, A; Lin, Y C Estrogen metabolism in primary kidney cell cultures from Syrian hamsters. Journal of steroid biochemistry. 1990 Jan; 36(4):325-31.
  • Li, P, K; Brueggemeier, R W Synthesis and biochemical studies of 7-substituted 4,6-androstadiene-3,17-diones as aromatase inhibitors. Journal of medicinal chemistry. 1990 Jan; 33(1):101-5.
  • Brueggemeier, R, W; Li, P, K; Chen, H, H; Moh, P, P; Katlic, N E Biochemical and pharmacological development of steroidal inhibitors of aromatase. The Journal of steroid biochemistry and molecular biology. 1990 Jan; 37(3):379-85.
  • Chen, H, H; Brueggemeier, R W Synthesis and biochemistry of fluorescent aromatase inhibitors. Steroids. 1990 Jan; 55(3):123-7.
  • Brueggemeier, R W Biochemical and molecular aspects of aromatase. Journal of enzyme inhibition. 1990 Jan; 4(2):101-11.
  • Brueggemeier, R, W; Katlic, N E Aromatase inhibition by an enzyme-activated irreversible inhibitor in human carcinoma cell cultures. Cancer research. 1990 Jan; 50(12):3652-6.
  • Brueggemeier, R, W; Singh, U Inhibition of rat liver microsomal estrogen 2-hydroxylase by 2-methoxyestrogens. Journal of steroid biochemistry. 1989 Jan; 33(4A):589-93.
  • Brueggemeier, R, W; Li, P K Effects of the aromatase inhibitor 7 alpha-(4'-amino)phenylthio-4-androstene-3,17-dione on 7,12-dimethylbenz(a)anthracene-induced mammary carcinoma in rats. Cancer research. 1988 Jan; 48(23):6808-10.
  • Brueggemeier, R, W; Katlic, N E Effects of the aromatase inhibitor 7 alpha-(4'-amino)phenylthio-4-androstene-3,17-dione in MCF-7 human mammary carcinoma cell culture. Cancer research. 1987 Jan; 47(17):4548-51.
  • Snider, C, E; Brueggemeier, R W Potent enzyme-activated inhibition of aromatase by a 7 alpha-substituted C19 steroid. The Journal of biological chemistry. 1987 Jan; 262(18):8685-9.
  • Brueggemeier, R, W; Bannan, R A Androgens inhibit the formation of catechol estrogens by estrogen 2-hydroxylase present in rat liver microsomal preparations. Journal of steroid biochemistry. 1986 Jan; 25(3):351-4.
  • Fung, Y, K; Brueggemeier, R, W; Uretsky, N J Modulation of apomorphine-induced climbing behavior by estradiol. Pharmacology, biochemistry, and behavior. 1986 Jan; 24(1):139-41.
  • Snider, C, E; Brueggemeier, R W Covalent modification of aromatase by a radiolabeled irreversible inhibitor. Journal of steroid biochemistry. 1985 Jan; 22(3):325-30.
  • Brueggemeier, R, W; Kimball, J, G; Kraft, F Estrogen metabolism in rat liver microsomal and isolated hepatocyte preparations--I. Metabolite formation and irreversible binding to cellular macromolecules. Biochemical pharmacology. 1984 Jan; 33(23):3853-9.
  • Brueggemeier, R, W; Kimball, J, G; Kraft, F Estrogen metabolism in rat liver microsomal and isolated hepatocyte preparations--II. Inhibition studies. Journal of steroid biochemistry. 1984 Jan; 21(6):709-16.
  • Brueggemeier, R W Inhibition of estrogen 2-hydroxylase. Journal of steroid biochemistry. 1983 Jan; 19(5):1683-5.
  • Brueggemeier, R, W; Kimball, J G Kinetics of inhibition of estrogen 2-hydroxylase by various haloestrogens. Steroids. 1983 Jan; 42(1):93-103.
  • Brueggemeier, R, W; Snider, C, E; Counsell, R E Substituted C19 steroid analogs as inhibitors of aromatase. Cancer research. 1982 Jan; 42(8 Suppl):3334s-3337s.
  • Brueggemeier, R, W; Snider, C, E; Kimball, J G A photoaffinity inhibitor of aromatase. Steroids. 1982 Jan; 40(6):679-89.
  • Brueggemeier, R W Kinetics of rat liver microsomal estrogen 2-hydroxylase. Evidence for sex differences at initial velocity conditions. The Journal of biological chemistry. 1981 Jan; 256(20):10239-42.
  • Brueggemeier, R, W; Floyd, E, E; Counsell, R E Synthesis and biochemical evaluation of inhibitors of estrogen biosynthesis. Journal of medicinal chemistry. 1978 Jan; 21(10):1007-11.