非雄激素竞争型雄激素受体拮抗剂设计策略

Design strategy of anti-androgen targeting the non-HBP sites of androgen receptor

雄激素受体(androgen receptor,AR)是前列腺癌治疗中最为重要的药物靶点,但抗雄激素药物在使用过程中产生的耐药性问题给前列腺癌患者的治疗带来了巨大挑战。本文回顾了雄激素受体的结构功能及传统治疗位点产生药物抗性的原因,并总结非雄激素竞争型的雄激素受体拮抗剂设计策略,为发展新型抗前列腺癌药物提供依据。

Androgen receptor （ AR } is the most important target for the therapy of prostate cancer. However, the drug resistance during the treatment becomes the greatest challenge. Herein, we gave an overview of the structure and functions of AR and the drug resistances due to the mutations in the HBP site.Then this article summarized the design strategy of the AR antagonists targeting the non-HBP sites of AR ,which should help to the development of novel anti-prostate cancer drugs.