Methoxychalcone inhibitors of androgen receptor translocation and function.
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ABSTRACT:
SUBMITTER: Kim YS
PROVIDER: S-EPMC3308679 | biostudies-literature | 2012 Mar
REPOSITORIES: biostudies-literature
Publications
Methoxychalcone inhibitors of androgen receptor translocation and function.
Kim Yeong Sang YS Kumar Vineet V Lee Sunmin S Iwai Aki A Neckers Len L Malhotra Sanjay V SV Trepel Jane B JB
Bioorganic & medicinal chemistry letters 20120121 5
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 ...[more]
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