Education

• Postdoctoral Fellow, Harvard Medical School, 1977-1979
• PhD, University of Michigan, 1977
• MS, University of Michigan, 1975
• BA, Michigan State University, 1972

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Areas of Interest

Aromatase Inhibitors, Steroid Biochemistry, Breast Cancer, Enzyme Inhibitors

The major research activities of Dr. Brueggemeier focus in the areas of steroid chemistry and biochemistry, hormones and cancer, medicinal chemistry, and radiochemistry. Research approaches involve the application of expertise in steroid chemistry/biochemistry to the examination of steroid biosynthesis, metabolism, and action at the molecular level. Results from these interdisciplinary investigations will aid in understanding the molecular and biochemical role(s) of estrogens in hormone-dependent cancers and in the development of new approaches to treatment of hormone-dependent cancers.

One research program focuses on the development of aromatase inhibitors for the treatment of estrogen-dependent breast cancer. Estrogens are biosynthesized from androgens by the cytochrome P450 enzyme complex called aromatase. Several inhibitors of aromatase have been studied, and several mechanism-based inhibitors are being utilized to probe the enzyme active site.

A second research project focuses on estrogens and estrogen metabolites and their roles in the development of certain estrogen-dependent cancers. One emphasis focuses on the biochemistry of the enzyme estrogen 2- and 4-hydroxylases and inhibition of the enzymes. A third project is the examination of the effects of these molecules on estrogen-induced responses in vitro and in vivo, with an emphasis on estrogen-induced growth factors in the TGFa and the FGF families and on growth inhibitory TGFb. A fourth research project focuses on examination of the breast cancer tissue microenvironment. The tissue microenvironment can influence the extent of estrogen biosynthesis and metabolism, result in altered levels of hormonally active estrogens and their metabolites, and therefore influence breast tumor development and growth. Biochemical and molecular examination of this hypothesis in vitro are being studied in human patient breast tissue specimens and in several human b reast cancer cell systems currently in use in the laboratories. The studies include examining the extent of aromatase (CYP19) expression and cyclooxygenase (COX-1 and COX-2) expression in human breast cancer specimens and determining the biological consequences of estrogen biosynthesis and metabolism in the human breast cell systems. Finally, a new research thrust in Dr. Brueggemeier's laboratory is the development of directed combinatorial libraries and bioassay evaluation of nonsteroidal agents as potential agonists or antagonists of steroid biochemistry in breast cancer. The molecular scaffold used in this research project is the benzopyranone ring system, present in a number of natural products such as flavonoids and isoflavonoids. The synthesis uses readily available starting materials, employs mild and high yielding reactions, and is amendable to rapid synthesis of diverse libraries.

[ View Recent Publications ]

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Previous Courses Taught

Pharmacy 410, 601, 735, 800

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Professional Experience

• 2003-present: Dean, College of Pharmacy, The Ohio State University, Columbus, Ohio.
• 1990-present: Professor, Division of Medicinal Chemistry and Pharmacognosy,
  College of Pharmacy, The Ohio State University, Columbus, Ohio.
• 1992-2003: Chairperson, Division of Medicinal Chemistry and Pharmacognosy,
  College of Pharmacy, The Ohio State University, Columbus, Ohio.
• 1985-1990: Associate Professor, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio.
• 1979-1985: Assistant Professor, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio.

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Related Links

Office of the Dean: http://www.pharmacy.ohio-state.edu/services/admin/dean/dean.cfm

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