期刊论文详细信息
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 卷:22
Methoxychalcone inhibitors of androgen receptor translocation and function
Article
Kim, Yeong Sang2  Kumar, Vineet1  Lee, Sunmin2  Iwai, Aki3  Neckers, Len3  Malhotra, Sanjay V.1  Trepel, Jane B.2 
[1] Natl Canc Inst Frederick, Lab Synthet Chem, Dev Therapeut Program Support, SAIC Frederick, Frederick, MD 21702 USA
[2] NCI, Med Oncol Branch, NIH, Bethesda, MD 20892 USA
[3] NCI, Urol Oncol Branch, NIH, Bethesda, MD 20892 USA
关键词: Chalcone;    Antiandrogen;    Androgen receptor translocation;    Prostate cancer;    Hsp90;   
DOI  :  10.1016/j.bmcl.2011.12.141
来源: Elsevier
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【 摘 要 】

Androgen receptor activity drives incurable castrate-resistant prostate cancer. All approved antiandrogens inhibit androgen receptor-driven transcription, and in addition the second-generation antiandrogen MDV3100 inhibits ligand-activated androgen receptor nuclear translocation, via an unknown mechanism. Here, we report methoxychalcones that lock the heat shock protein 90-androgen receptor complex in the cytoplasm in an androgen-non-responsive state, thus demonstrating a novel chemical scaffold for antiandrogen development and a unique mechanism of antiandrogen activity. Published by Elsevier Ltd.

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