Androgen receptor inhibitors in treating prostate cancer  

作　　者：Ryan N Cole Qinghua Fang Kanako Matsuoka Zhou Wang 

机构地区：[1]Department of Urology,University of Pittsburgh School of Medicine,Pittsburgh,PA 15232,USA [2]UPMC Hillman Cancer Center,University of Pittsburgh School of Medicine,Pittsburgh,PA 15232,USA [3]Department of Pharmacology and Chemical Biology,University of Pittsburgh School of Medicine,Pittsburgh,PA 15213,USA

出　　处：《Asian Journal of Andrology》2025年第2期144-155,共12页亚洲男性学杂志(英文版)

基　　金：supported in part by DOD Idea Development Award(HT9425-23-1-0295);NIH grants(R01 CA265897 and R21 CA280467);by the Department of Urology,University of Pittsburgh School of Medicine,Pittsburgh,PA,USA。

摘　　要：Androgens play an important role in prostate cancer development and progression.Androgen action is mediated through the androgen receptor(AR),a ligand-dependent DNA-binding transcription factor.AR is arguably the most important target for prostate cancer treatment.Current USA Food and Drug Administration(FDA)-approved AR inhibitors target the ligand-binding domain(LBD)and have exhibited efficacy in prostate cancer patients,particularly when used in combination with androgen deprivation therapy.Unfortunately,patients treated with the currently approved AR-targeting agents develop resistance and relapse with castration-resistant prostate cancer(CRPC).The major mechanism leading to CRPC involves reactivation of AR signaling mainly through AR gene amplification,mutation,and/or splice variants.To effectively inhibit the reactivated AR signaling,new approaches to target AR are being actively explored.These new approaches include novel small molecule inhibitors targeting various domains of AR and agents that can degrade AR.The present review provides a summary of the existing FDA-approved AR antagonists and the current development of some of the AR targeting agents.

关 键 词：androgen receptor ANTI-ANDROGENS prostate cancer 

分 类 号：R737.25[医药卫生—肿瘤]