ROBERT BRUEGGEMEIER

Summary

Affiliation: The Ohio State University
Country: USA

Publications

  1. ncbi request reprint Aromatase inhibition in JAr choriocarcinoma cells by 7alpha-arylaliphatic androgens
    R W Brueggemeier
    College of Pharmacy, The Ohio State University, Columbus 43210, U S A
    J Steroid Biochem Mol Biol 61:73-7. 1997
  2. ncbi request reprint Translational studies on aromatase, cyclooxygenases, and enzyme inhibitors in breast cancer
    Robert W Brueggemeier
    College of Pharmacy, The Ohio State University, 500 W 12th Avenue, Columbus, OH 43210, USA
    J Steroid Biochem Mol Biol 95:129-36. 2005
  3. ncbi request reprint Aromatase inhibitors in the treatment of breast cancer
    Robert W Brueggemeier
    College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, Ohio 43210 1291, USA
    Endocr Rev 26:331-45. 2005
  4. ncbi request reprint Update on the use of aromatase inhibitors in breast cancer
    Robert W Brueggemeier
    Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, OH 43210, USA
    Expert Opin Pharmacother 7:1919-30. 2006
  5. ncbi request reprint Aromatase and cyclooxygenases: enzymes in breast cancer
    Robert W Brueggemeier
    Division of Medical Chemistry and Pharmacognosy, OSU Comprehensive Cancer Center, College of Pharmacy, The Ohio State University, 500 W 12th Avenue, Columbus, OH 43210 1291, USA
    J Steroid Biochem Mol Biol 86:501-7. 2003
  6. pmc Aromatase and COX in breast cancer: enzyme inhibitors and beyond
    Robert W Brueggemeier
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, OH 43210, USA
    J Steroid Biochem Mol Biol 106:16-23. 2007
  7. ncbi request reprint Relationship between aromatase and cyclooxygenases in breast cancer: potential for new therapeutic approaches
    R W Brueggemeier
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
    Minerva Endocrinol 31:13-26. 2006
  8. ncbi request reprint Overview of the pharmacology of the aromatase inactivator exemestane
    Robert W Brueggemeier
    College of Pharmacy, The Ohio State University, Columbus 43210 1291, USA
    Breast Cancer Res Treat 74:177-85. 2002
  9. ncbi request reprint Aromatase inhibitors in breast cancer therapy
    Robert W Brueggemeier
    Ohio State University, 500 West 12th Avenue, Columbus, OH 43210, USA
    Expert Rev Anticancer Ther 2:181-91. 2002
  10. ncbi request reprint Aromatase, aromatase inhibitors, and breast cancer
    R W Brueggemeier
    Medicinal Chemistry and Pharmacognosy, College of Pharmacy, and Hormones and Cancer Program, Comprehensive Cancer Center, The Ohio State University, Columbus, OH 43210, USA
    Am J Ther 8:333-44. 2001

Research Grants

  1. ESTROGEN BIOTRANSFORMATIONS AND BREAST CANCER ETIOLOGY
    ROBERT BRUEGGEMEIER; Fiscal Year: 2002
  2. ESTROGEN BIOTRANSFORMATIONS AND BREAST CANCER ETIOLOGY
    ROBERT BRUEGGEMEIER; Fiscal Year: 2006

Collaborators

Detail Information

Publications44

  1. ncbi request reprint Aromatase inhibition in JAr choriocarcinoma cells by 7alpha-arylaliphatic androgens
    R W Brueggemeier
    College of Pharmacy, The Ohio State University, Columbus 43210, U S A
    J Steroid Biochem Mol Biol 61:73-7. 1997
    ....
  2. ncbi request reprint Translational studies on aromatase, cyclooxygenases, and enzyme inhibitors in breast cancer
    Robert W Brueggemeier
    College of Pharmacy, The Ohio State University, 500 W 12th Avenue, Columbus, OH 43210, USA
    J Steroid Biochem Mol Biol 95:129-36. 2005
    ....
  3. ncbi request reprint Aromatase inhibitors in the treatment of breast cancer
    Robert W Brueggemeier
    College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, Ohio 43210 1291, USA
    Endocr Rev 26:331-45. 2005
    ..Use of an aromatase inhibitor as initial therapy or after treatment with tamoxifen is now recommended as adjuvant hormonal therapy for a postmenopausal woman with hormone-dependent breast cancer...
  4. ncbi request reprint Update on the use of aromatase inhibitors in breast cancer
    Robert W Brueggemeier
    Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, OH 43210, USA
    Expert Opin Pharmacother 7:1919-30. 2006
    ..Recently published results show improved responses with these agents compared with tamoxifen...
  5. ncbi request reprint Aromatase and cyclooxygenases: enzymes in breast cancer
    Robert W Brueggemeier
    Division of Medical Chemistry and Pharmacognosy, OSU Comprehensive Cancer Center, College of Pharmacy, The Ohio State University, 500 W 12th Avenue, Columbus, OH 43210 1291, USA
    J Steroid Biochem Mol Biol 86:501-7. 2003
    ..Thus, the regulation of both enzymes in breast cancer involves complex paracrine interactions, resulting in significant consequences on the pathogenesis of breast cancer...
  6. pmc Aromatase and COX in breast cancer: enzyme inhibitors and beyond
    Robert W Brueggemeier
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, OH 43210, USA
    J Steroid Biochem Mol Biol 106:16-23. 2007
    ..Thus, these results suggest that the siRNAs and novel sulfonanilides targeting aromatase expression may be valuable tools for selective regulation of aromatase in breast cancer...
  7. ncbi request reprint Relationship between aromatase and cyclooxygenases in breast cancer: potential for new therapeutic approaches
    R W Brueggemeier
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
    Minerva Endocrinol 31:13-26. 2006
    ..Thus, PGE2 produced by COX enzymes may act locally in paracrine and autocrine fashion to increase the biosynthesis of estrogen by aromatase in hormone-dependent breast cancer development...
  8. ncbi request reprint Overview of the pharmacology of the aromatase inactivator exemestane
    Robert W Brueggemeier
    College of Pharmacy, The Ohio State University, Columbus 43210 1291, USA
    Breast Cancer Res Treat 74:177-85. 2002
    ..Current findings suggest that exemestane will be a valuable alternative for women with breast cancer, not only for those progressing on other hormonal therapies but in earlier stages of the disease and prevention...
  9. ncbi request reprint Aromatase inhibitors in breast cancer therapy
    Robert W Brueggemeier
    Ohio State University, 500 West 12th Avenue, Columbus, OH 43210, USA
    Expert Rev Anticancer Ther 2:181-91. 2002
    ....
  10. ncbi request reprint Aromatase, aromatase inhibitors, and breast cancer
    R W Brueggemeier
    Medicinal Chemistry and Pharmacognosy, College of Pharmacy, and Hormones and Cancer Program, Comprehensive Cancer Center, The Ohio State University, Columbus, OH 43210, USA
    Am J Ther 8:333-44. 2001
    ....
  11. ncbi request reprint Correlation of aromatase and cyclooxygenase gene expression in human breast cancer specimens
    R W Brueggemeier
    College of Pharmacy, The Ohio State University, Columbus 43210 1291, USA
    Cancer Lett 140:27-35. 1999
    ....
  12. ncbi request reprint Biochemistry and pharmacology of 7alpha-substituted androstenediones as aromatase inhibitors
    R W Brueggemeier
    The College of Pharmacy and The OSU Comprehensive Cancer Center, The Ohio State University, Columbus 43210, U S A
    J Steroid Biochem Mol Biol 61:247-54. 1997
    ..The size of the 7alpha-substituent influences optimal binding of steroidal inhibitors to the active site and affects the extent of enzyme-mediated inactivation observed with androsta-1,4-diene-3,17-dione analogs...
  13. ncbi request reprint 2-Methoxymethylestradiol: a new 2-methoxy estrogen analog that exhibits antiproliferative activity and alters tubulin dynamics
    R W Brueggemeier
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, OH 43210 1291, USA
    J Steroid Biochem Mol Biol 78:145-56. 2001
    ..Thus, 2-MeOMeE(2) is an estrogen analog with minimal estrogenic properties that demonstrates antiproliferative effects both in vitro and in the human xenograft animal model of human breast cancer...
  14. ncbi request reprint Effects of phytoestrogens and synthetic combinatorial libraries on aromatase, estrogen biosynthesis, and metabolism
    R W Brueggemeier
    College of Pharmacy and OSU Comprehensive Cancer Center, The Ohio State University, Columbus 43210, USA
    Ann N Y Acad Sci 948:51-66. 2001
    ..Several compounds in the initial libraries have demonstrated moderate aromatase inhibitory activity in screening assays...
  15. pmc Selective regulation of aromatase expression for drug discovery
    Robert W Brueggemeier
    College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
    J Steroid Biochem Mol Biol 118:207-10. 2010
    ..Thus, these results suggest that the novel sulfonanilides and the siRNAs targeting aromatase expression may be valuable tools for selective regulation of aromatase in breast cancer...
  16. ncbi request reprint Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition
    Bin Su
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 W 12th Avenue, Columbus, Ohio 43210, USA
    J Med Chem 49:1413-9. 2006
    ..These studies suggest that the novel sulfonanilide compounds suppress aromatase activity and transcription in SK-BR-3 breast cancer cells independent of COX-2 inhibition...
  17. pmc Suppression of aromatase in human breast cells by a cyclooxygenase-2 inhibitor and its analog involves multiple mechanisms independent of cyclooxygenase-2 inhibition
    Bin Su
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
    Steroids 73:104-11. 2008
    ..These results suggest that NS-398 and its N-methyl analog suppress aromatase expression and activity with multiple mechanisms...
  18. ncbi request reprint Synthesis and biological evaluation of selective aromatase expression regulators in breast cancer cells
    Bin Su
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, and Ohio State Biochemistry Program, The Ohio State University, 500 W 12th Avenue, Columbus, Ohio 43210, USA
    J Med Chem 50:1635-44. 2007
    ..Also, the sulfonanilide compounds selectively decrease aromatase gene expression in breast cancer cells, without exhibiting cytotoxic or apoptotic effects at low micromole concentrations...
  19. ncbi request reprint Lead optimization of 7-benzyloxy 2-(4'-pyridylmethyl)thio isoflavone aromatase inhibitors
    Bin Su
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, 43210, USA
    Bioorg Med Chem 13:6571-7. 2005
    ..Data supporting the ability of these analogs to suppress aromatase enzyme activity in the SK-BR-3 breast cancer cell line are also presented...
  20. ncbi request reprint Interrelationships between cyclooxygenases and aromatase: unraveling the relevance of cyclooxygenase inhibitors in breast cancer
    Edgar S Diaz-Cruz
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA
    Anticancer Agents Med Chem 6:221-32. 2006
    ..Thus, PGE(2) produced via COX may act locally in paracrine and autocrine fashion to increase the biosynthesis of estrogen by aromatase in hormone-dependent breast cancer development...
  21. pmc Synthesis and biological evaluation of novel sulfonanilide compounds as antiproliferative agents for breast cancer
    Bin Su
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, 500 West 12th Avenue, The Ohio State University, Columbus, OH 43210, USA
    J Comb Chem 10:475-83. 2008
    ..Structure-function analysis indicated that the inhibition of cell growth by compounds derived from the novel sulfonanilides required a bulky terminal phenyl ring, a methanesulfonamide, and a hydrophobic carboxamide moiety...
  22. ncbi request reprint Cyclooxygenase inhibitors suppress aromatase expression and activity in breast cancer cells
    Edgar S Diaz-Cruz
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA
    J Clin Endocrinol Metab 90:2563-70. 2005
    ....
  23. ncbi request reprint Synthesis and characterization of azole isoflavone inhibitors of aromatase
    John C Hackett
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 W 12th Avenue, Columbus, OH 43210, USA
    Bioorg Med Chem 13:4063-70. 2005
    ..In addition, difference binding spectra of inhibitors to immunoaffinity-purified aromatase produces classical Type II spectra consistent with coordination of the nitrogen lone pair electrons to the aromatase P450 heme...
  24. ncbi request reprint Aromatase inhibitors: new endocrine treatment of breast cancer
    Robert W Brueggemeier
    Medicinal Chemistry and Pharmacognosy, College of Pharmacy, and Hormones and Cancer Program, OSU Comprehensive Cancer Center, The Ohio State University, Columbus, Ohio 43210, USA
    Semin Reprod Med 22:31-43. 2004
    ..Several clinical studies of aromatase inhibitors are currently focusing on the use of these agents in the adjuvant setting for the treatment of early breast cancer...
  25. doi request reprint Novel sulfonanilide analogs decrease aromatase activity in breast cancer cells: synthesis, biological evaluation, and ligand-based pharmacophore identification
    Bin Su
    College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA
    J Med Chem 51:1126-35. 2008
    ..The results suggest that both genomic and nongenomic mechanisms of these compounds are involved within the aromatase suppression effect...
  26. doi request reprint 4-Hydroxyphenylretinamide (4HPR) derivatives regulate aromatase activity and expression in breast cancer cells
    Bin Su
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500W 12th Avenue, Columbus, OH 43210, USA
    J Steroid Biochem Mol Biol 109:40-6. 2008
    ..Placental microsomal aromatase assay rule out the possibility that this compound directly inhibits the aromatase enzyme. A non-genomic mechanism in suppression of cellular aromatase activity of this compound is proposed...
  27. doi request reprint Transferrin-conjugated lipid-coated PLGA nanoparticles for targeted delivery of aromatase inhibitor 7alpha-APTADD to breast cancer cells
    Yu Zheng
    Division of Pharmaceutics, College of Pharmacy, Ohio State University, Columbus, OH 43210, USA
    Int J Pharm 390:234-41. 2010
    ..In conclusion, Tf-conjugated lipid-coated PLGA nanoparticles are potential vehicles for improving the efficiency and specificity of therapeutic delivery of aromatase inhibitors...
  28. ncbi request reprint Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones
    Young Woo Kim
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, Ohio 43210, USA
    J Med Chem 47:4032-40. 2004
    ..In this paper, we describe the design, synthesis, and biological evaluation of a novel series of 2-(4'-pyridylmethyl)thioisoflavones as the first example of synthetic isoflavone-based aromatase inhibitors...
  29. ncbi request reprint The final catalytic step of cytochrome p450 aromatase: a density functional theory study
    John C Hackett
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, Ohio 43210, USA
    J Am Chem Soc 127:5224-37. 2005
    ..These calculations support a dehydrogenase behavior of aromatase in the final catalytic step, which can be summarized by 1beta-hydrogen atom abstraction followed by gem-diol deprotonation...
  30. ncbi request reprint Signaling pathways regulating aromatase and cyclooxygenases in normal and malignant breast cells
    Jeanette A Richards
    Ohio State Biochemistry Program, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
    J Steroid Biochem Mol Biol 80:203-12. 2002
    ....
  31. ncbi request reprint Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay
    Marcy J Balunas
    Program for Collaborative Research in the Pharmaceutical Sciences and Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60612, USA
    J Nat Prod 69:700-3. 2006
    ..In natural product screening efforts, especially using plant seeds, it is recommended that extracts active in noncellular bioassays should be dereplicated for the presence of fatty acids prior to bioassay-guided fractionation...
  32. ncbi request reprint Overcoming trastuzumab resistance in HER2-overexpressing breast cancer cells by using a novel celecoxib-derived phosphoinositide-dependent kinase-1 inhibitor
    Ping Hui Tseng
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, 336 Parks Hall, The Ohio State University, 500 West 12th Avenue, Columbus, 43210 1291, USA
    Mol Pharmacol 70:1534-41. 2006
    ..This combination treatment represents a novel strategy to increase the efficacy of trastuzumab and to overcome trastuzumab resistance in the treatment of HER2-positive breast cancer...
  33. ncbi request reprint Prostaglandin E2 regulates aromatase activity and expression in human adipose stromal cells via two distinct receptor subtypes
    Jeanette A Richards
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Ohio State University, Columbus, Ohio 43210, USA
    J Clin Endocrinol Metab 88:2810-6. 2003
    ..Collectively, the results demonstrate that regulation of aromatase by PGE(2) is complex and may influence the development and progression of hormone-dependent breast cancer...
  34. doi request reprint Sensitizing estrogen receptor-negative breast cancer cells to tamoxifen with OSU-03012, a novel celecoxib-derived phosphoinositide-dependent protein kinase-1/Akt signaling inhibitor
    Shu Chuan Weng
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 336 L M Parks Hall, 500 West 12th Avenue, Columbus, OH 43210, USA
    Mol Cancer Ther 7:800-8. 2008
    ..Considering the urgent need for novel therapeutic strategies for ER-negative breast cancer patients, this combinatorial approach is worthy of continued investigation...
  35. pmc Evaluation of synthetic isoflavones on cell proliferation, estrogen receptor binding affinity, and apoptosis in human breast cancer cells
    Danyetta D Davis
    Ohio State Biochemistry Program, College of Medicine, The Ohio State University, 318 West 12th Avenue, Columbus, OH 43210, USA
    J Steroid Biochem Mol Biol 108:23-31. 2008
    ..Thus, the synthetic trisubstituted isoflavones act on multiple signaling pathways leading to activation of mechanisms of cell-death and ultimately affecting breast cancer cell survival...
  36. ncbi request reprint Estrogen receptor-mediated regulation of oxidative stress and DNA damage in breast cancer
    James A Mobley
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University Comprehensive Cancer Center, The Ohio State University, Columbus, OH 43210, USA
    Carcinogenesis 25:3-9. 2004
    ..In addition, this is the first report indicating that E2 is capable of inducing an increase in sensitivity to oxidative DNA damage through an ER-mediated mechanism...
  37. ncbi request reprint Synthesis and estrogen receptor binding affinities of 7-hydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-ones containing a basic side chain
    Young Woo Kim
    Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus 43210, USA
    Bioorg Med Chem Lett 13:1475-8. 2003
    ..These compounds also displayed selectivity for ERalpha over ERbeta...
  38. pmc Increased proteasome-dependent degradation of estrogen receptor-alpha by TGF-beta1 in breast cancer cell lines
    Trevor A Petrel
    The Ohio State Biochemistry Program, College of Medicine and Public Health, and OSU Comprehensive Cancer Center, The Ohio State University, Columbus, Ohio 43210, USA
    J Cell Biochem 88:181-90. 2003
    ..Collectively, this data supports a role for TGF-beta1 in regulating the growth of otherwise insensitive breast cancer cells through modulation of ERalpha stability...
  39. ncbi request reprint Role of the azinomycin naphthoate and central amide in sequence-dependent DNA alkylation and cytotoxicity of epoxide-bearing substructures
    Robert S Coleman
    Department of Chemistry, The Ohio State University, 100 West 18th Avenue, Columbus, Ohio 43210, USA
    Org Lett 4:3545-8. 2002
    ..g., 2). Compounds were evaluated for cytotoxicity against two breast cancer cell lines. [structure: see text]..
  40. ncbi request reprint Increasing the DNA damage threshold in breast cancer cells
    James A Mobley
    Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University, Columbus, Ohio 43210, USA
    Toxicol Appl Pharmacol 180:219-26. 2002
    ....
  41. pmc Xanthones from the botanical dietary supplement mangosteen (Garcinia mangostana) with aromatase inhibitory activity
    Marcy J Balunas
    Department of Medicinal Chemistry and Pharmacognosy, Program for Collaborative Research in the Pharmaceutical Sciences, College of Pharmacy, University of Illinois at Chicago, Chicago, Illinois 60612, USA
    J Nat Prod 71:1161-6. 2008
    ....
  42. pmc Natural products as aromatase inhibitors
    Marcy J Balunas
    Program for Collaborative Research in the Pharmaceutical Sciences and Department of Medical Chemistry and Pharnacognosy, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60612, USA
    Anticancer Agents Med Chem 8:646-82. 2008
    ..A thorough review of the literature regarding natural product extracts and secondary metabolites of plant, microbial, and marine origin that have been shown to exhibit aromatase inhibitory activity is presented herein...
  43. ncbi request reprint Peroxisome proliferator-activated receptor gamma-independent ablation of cyclin D1 by thiazolidinediones and their derivatives in breast cancer cells
    Jui Wen Huang
    College of Pharmacy, The Ohio State University, 336 L M Parks Hall, Columbus, OH 43210, USA
    Mol Pharmacol 67:1342-8. 2005
    ....
  44. ncbi request reprint Development of keratinocyte growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
    John Hackett
    Department of Pharmaceutical Sciences, College of Pharmacy, University of Oklahoma, Health Sciences Center, Oklahoma City, Oklahoma 73117, USA
    Anticancer Res 27:3801-6. 2007
    ..Receptor modeling of KGFR was used to identify selective KGFR tyrosine kinase inhibitor (TKI) molecules with high receptor affinity. The present study describes the synthesis and biological activity of three of the KGFR TKI compounds...

Research Grants10

  1. ESTROGEN BIOTRANSFORMATIONS AND BREAST CANCER ETIOLOGY
    ROBERT BRUEGGEMEIER; Fiscal Year: 2002
    ....
  2. ESTROGEN BIOTRANSFORMATIONS AND BREAST CANCER ETIOLOGY
    ROBERT BRUEGGEMEIER; Fiscal Year: 2006
    ..3) To measure cellular levels of aromatase expression and cyclooxygenases expression in human breast cancer specimens. ..