前列腺癌小分子降解雄激素受体的研究

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

Volume: 18 Issue: 7

关键词: 耐药机制，雄激素受体，降解，前列腺癌，小分子，新策略。

摘要: 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:

Degradation of Androgen Receptor through Small Molecules for Prostate Cancer, Current Cancer Drug Targets 2018; 18 (7) . https://dx.doi.org/10.2174/1568009617666171107103936