蛋白精氨酸甲基转移酶5抑制剂研究进展  

Research progress of protein arginine methyltransferase 5 inhibitors

作　　者：詹康宁 全旭 黄张建[1] 赵立文 ZHAN Kangning;QUAN Xu;HUANG Zhangjian;ZHAO Liwen(Center of Drug Discovery,China Pharmaceutical University,Nanjing 210009;Nanjing Sanhome Pharmaceutical Co.,Ltd.,Nanjing 210038,China)

机构地区：[1]中国药科大学新药研究中心,南京210009 [2]南京圣和药业股份有限公司,南京210038

出　　处：《中国药科大学学报》2021年第3期371-378,共8页Journal of China Pharmaceutical University

摘　　要：蛋白精氨酸甲基转移酶(PRMTs)对组蛋白和非组蛋白的翻译后修饰在生物学过程中起到了非常重要的作用。PRMT5是精氨酸残基对称双甲基化的主要酶,已被视为肿瘤治疗的潜在靶点。在过去10年中,发现和开发PRMT5抑制剂已经成为科研人员关注的热点。本文介绍了PRMT5的结构、生化功能以及其与肿瘤的相关性,同时就目前在研的PRMT5抑制剂与其结合方式以及生物活性进行综述,并讨论了PRMT5抑制剂在肿瘤治疗中的应用潜力。Protein arginine methyltransferases,which proceed the post-translational modification of both his-tones and non-histones,play an important role in many biological pathways.Protein arginine methyltransferase 5(PRMT5)is a major enzyme responsible for symmetric di-methylation of arginine residues and has been suggestedas a potential therapeutic target for tumors.In the past decade,the discovery and development of PRMT5 inhibi-tors have become one of the most important research fields.This article introduces the structure and biochemicalfunction of PRMT5 and its correlation with cancer reviews,the binding modes and biological data of PRMT5 inhibitors under development,and discusses the clinical application potential of PRMT5 inhibitors in the treat-ment of cancer.

关 键 词：蛋白精氨酸甲基转移酶5 小分子抑制剂 表观遗传 精氨酸甲基化 抗肿瘤靶点 

分 类 号：R914[医药卫生—药物化学]