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 | |
【 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.
【 授权许可】
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【 预 览 】
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