Article
Galeterone prevents androgen receptor binding to chromatin and enhances degradation of mutant androgen receptor.
Clinical cancer research : an official journal of the American Association for Cancer Research - 1 Aug 2014
Yu Ziyang, Cai Changmeng, Gao Shuai, Simon Nicholas I, Shen Howard C, Balk Steven P
Abstract excerpt
PURPOSE: Galeterone inhibits the enzyme CYP17A1 and is currently in phase II clinical trials for castration-resistant prostate cancer (CRPC). Galeterone is also a direct androgen receptor (AR) antagonist and may enhance AR degradation. This study was undertaken to determine the molecular basis for AR effects and their therapeutic potential. EXPERIMENTAL DESIGN: Effects of galeterone on AR expression and...
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