Selective regulation of aromatase expression for drug discovery.

The Journal of Steroid Biochemistry and Molecular Biology
R W BrueggemeierYasuro Sugimoto

Abstract

Aromatase is a particularly attractive drug target in the treatment of hormone-responsive breast cancer, and aromatase activity in breast cancer patients is greater in or near the tumor tissue compared with the normal breast tissue. Complex regulation of aromatase expression in human tissues involves alternative promoter sites that provide tissue-specific control. Previous studies in our laboratories suggested a strong association between aromatase (CYP19) gene expression and the expression of cyclooxygenase (COX) genes. Additionally, COX selective inhibitors can suppress CYP19 gene expression and decrease aromatase activity. Our current hypothesis is that pharmacological regulation of aromatase can act locally to decrease the biosynthesis of estrogen and may provide additional therapy options for patients with hormone-dependent breast cancer. Two pharmacological approaches are being developed, one approach utilizing small molecule drug design and the second approach involving mRNA silencing technology. The small molecule drug design approach focuses on the synthesis and biological evaluation of a novel series of sulfonanilide analogs derived from COX-2 selective inhibitors. Combinatorial chemistry approaches were used to gener...Continue Reading

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Jul 10, 2007·The Journal of Steroid Biochemistry and Molecular Biology·Robert W BrueggemeierDanyetta D Davis

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Citations

Sep 1, 2011·Chinese Journal of Cancer Research = Chung-kuo Yen Cheng Yen Chiu·Xue-Song Fu, Ping-Ping Li
Dec 14, 2011·Molecular Pharmaceutics·Chenguang ZhouRobert J Lee
Jun 23, 2011·Reproductive Biology and Endocrinology : RB&E·Shabana I KhanAsok K Dasmahapatra
Sep 26, 2009·The Journal of Steroid Biochemistry and Molecular Biology·Anita K DunbierMelanie R Palomares

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