Methoxychalcone inhibitors of androgen receptor translocation and function

Yeong Sang Kim, Vineet Kumar, Sunmin Lee, Aki Iwai, Len Neckers, Sanjay V. Malhotra, Jane B. Trepel

Research output: Contribution to journalArticlepeer-review

16 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)2105-2109
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number5
DOIs
StatePublished - Mar 1 2012
Externally publishedYes

Keywords

  • Androgen receptor translocation
  • Antiandrogen
  • Chalcone
  • Hsp90
  • Prostate cancer

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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