期刊
EXPERT OPINION ON DRUG DISCOVERY
卷 2, 期 10, 页码 1341-1355出版社
TAYLOR & FRANCIS LTD
DOI: 10.1517/17460441.2.10.1341
关键词
AF2; androgen-independent prostate cancer; antiandrogens; androgen receptor; co-activator-binding pocket; co-activators; ligand-binding pocket; surface inhibitors
The androgen receptor (AR) regulates gene transcription in many tissues and is profoundly important in prostate cancer. Antiandrogens compete with the natural hormone and are front line therapeutics to treat prostate cancer. However, antiandrogens frequently become ineffective after prolonged treatment because of development of tumor resistance. This paper reviews design principles for new generations of antiandrogens: super antagonists and surface allosteric modulators. Super antiandrogens are compounds with higher binding affinity than natural agonists and that contain precisely engineered hydrophobic groups that disrupt AR function. AR surface is also an attractive alternative target. Surface inhibitors are small molecules that directly block the receptor-co-activator interface, preventing co-activator recruitment. The challenges to designing these compounds are significant but so is the potential for treatment of the disease.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据