Recent advances in allosteric androgen receptor inhibitors for the potential treatment of castration-resistant prostate cancer

Guillermo Martinez-Ariza, Christopher Hulme

Research output: Contribution to journalReview articlepeer-review

4 Scopus citations

Abstract

Prostate cancer (PC) is the second most frequent cause of male cancer death in the USA. As such, the androgen receptor (AR) plays a crucial role in PC, making AR the major therapeutic target for PC. Current antiandrogen chemotherapy prevents androgen binding to the ligand-binding pocket (LBP) of AR. However, PC frequently recurs despite treatment and it progresses to castration-resistant prostate cancer. Behind this regression is renewed AR signaling initiated via mutations in the LBP. Hence, there is a critical need to improve the therapeutic options to regulate AR activity in sites other than the LBP. Herein, recently disclosed (2010-2015) allosteric AR inhibitors are summarized and a perspective on the potential pharmaceutical intervention at these sites is provided.

Original languageEnglish (US)
Pages (from-to)387-402
Number of pages16
JournalPharmaceutical patent analyst
Volume4
Issue number5
DOIs
StatePublished - Jan 1 2015

ASJC Scopus subject areas

  • Medicine(all)

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