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Bioorg Med Chem Lett. 2012 Mar 1;22(5):2105-9. doi: 10.1016/j.bmcl.2011.12.141. Epub 2012 Jan 21.

Methoxychalcone inhibitors of androgen receptor translocation and function.

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  • 1Medical Oncology Branch, National Cancer Institute, National Institutes of Health, 10 Center Drive, Bethesda, MD 20892, United States.

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.

Published by Elsevier Ltd.

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