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.

SUBMITTER: Kim YS 

PROVIDER: S-EPMC3308679 | biostudies-literature | 2012 Mar

REPOSITORIES: biostudies-literature