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Pharm Pat Anal. 2015;4(5):387-402. doi: 10.4155/ppa.15.20. Epub 2015 Sep 21.

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

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Department of Pharmacology & Toxicology, The University of Arizona, Biological Sciences West Room #351, 1041 E Lowell St, Tucson, AZ 85721, USA.
Department of Chemistry & Biochemistry, The University of Arizona, Tucson, AZ 85721, USA.


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.

[Indexed for MEDLINE]

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