Degradation of Androgen Receptor through Small Molecules for Prostate Cancer

Title:Degradation of Androgen Receptor through Small Molecules for Prostate Cancer

Volume: 18 Issue: 7

Author(s): Raoling Ge, Xi Xu, Pengfei Xu, Lei Li, Zhiyu Li*Jinlei Bian*

Affiliation:

• Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009,China

• Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009,China

Keywords: Resistance mechanism, androgen receptor, degradation, prostate cancer, small molecules, new strategies.

Abstract: Prostate cancer is the most common carcinoma among aged males in western countries and more aggressive and lethal castration resistant prostate cancer often occurs after androgen deprivation therapy. The high expression of androgens and androgen receptor is closely related to prostate cancer. Efficient androgen receptor antagonists, such as enzalutamide and ARN-509, could be employed as potent anti-prostate cancer agents. Nevertheless, recent studies have revealed that F876L mutation in androgen receptor converts the action of enzalutamide and ARN-509 from an antagonist to agonist, so that novel strategies are urgent to address this resistance mechanism. In this review, we focus on the discussion about some novel strategies, which targets androgen receptor mainly through the degrading pathway as potential treatments for prostate cancer.

Cite this article as:

Ge Raoling , Xu Xi , Xu Pengfei , Li Lei , Li Zhiyu *, Bian Jinlei *, Degradation of Androgen Receptor through Small Molecules for Prostate Cancer, Current Cancer Drug Targets 2018; 18 (7) . https://dx.doi.org/10.2174/1568009617666171107103936