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Methoxychalcone inhibitors of androgen receptor translocation and function.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kim YS,Kumar V,Lee S,Iwai A,Neckers L,Malhotra SV,Trepel JB

doi

10.1016/j.bmcl.2011.12.141

subject

Has Abstract

pub_date

2012-03-01 00:00:00

pages

2105-9

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00030-3

journal_volume

22

pub_type

杂志文章

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