抗前列腺癌相关核受体及小分子药物研究进展  

Advances in Anti-prostate Cancer-Related Nuclear Receptors and Small Molecule Drugs

作　　者：卢志芳 吴桐 吴锡山 李俊骅 张岩 刘洋[1] 翟鑫[1] 许永 LU Zhifang;WU Tong;WU Xishan;LI Junhua;ZHANG Yan;LIU Yang;ZHAI Xin;XU Yong(Key Laboratory of Structure-Based Drug Design and Discovery,Ministry of Education,Shenyang Pharmaceutical University,Shenyang 110016,China;Center for Chemical Biology and Drug Discovery,Guangzhou Institutes of Biomedicine and Health,Chinese Academy of Sciences,Guangzhou 510530,China)

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016 [2]中国科学院广州生物医药与健康研究院化学生物学与药物研究中心,广东广州510530

出　　处：《药学进展》2023年第8期593-607,共15页Progress in Pharmaceutical Sciences

基　　金：国家重点研发计划项目(No.2019YFE0123700);国家自然科学基金面上项目(No.82173745);广州市科技计划项目(No.202201010138)。

摘　　要：前列腺癌是男性高发和高致死的恶性肿瘤,其发生发展与雄激素受体(androgen receptor,AR)信号通路关联密切。AR基因扩增、突变和剪接变体表达等使得前列腺癌治疗面临耐药难题。开发新靶点以克服临床耐药是该领域亟需解决的关键问题。已有研究表明,除AR之外的其他核受体成员也和前列腺癌的发生发展密切相关。针对这些核受体开发的抗前列腺癌小分子药物已进入临床前或临床研究。综述这些核受体在前列腺癌中的作用机制及其相关小分子化合物的研究进展。Prostate cancer is a malignant tumor with an extremely high rate of incidence and mortality in male.The occurrence and development of prostate cancer are closely related to androgen receptor(AR)-mediated signaling pathway.AR gene amplification,mutation and splice variant expression have posed the problem of drug resistance for the treatment of prostate cancer.Therefore,it is urgent to discover novel targets to overcome clinical drug resistance of prostate cancer.Studies have shown that,besides AR,other members of the nuclear receptors are also closely related to the occurrence and progression of prostate cancer.Small molecule drugs targeting these nuclear receptors against prostate cancer have been studied in preclinical or clinical research.This paper reviews the mechanisms of action of these nuclear receptors in prostate cancer and the research progress of related small molecule compounds.

关 键 词：核受体 小分子化合物 前列腺癌 作用机制 

分 类 号：R914.2[医药卫生—药物化学] R979.1[医药卫生—药学]