PROTAC蛋白靶向嵌合体在抗肿瘤药物开发中研究进展  

Research Progress in PROTAC in the Development of Anti-tumor Drugs

作　　者：端木彦涛 胥骞 夏宇 曹建中 卢茂芳[1] 王福东[1] 彭东明[1] Duanmu Yantao;Xu Qian;Xia Yu;Cao Jianzhong;Lu Maofang;Wang Fudong;Peng Dongming(College of Pharmacy,Hunan University of Chinese Medicine,Changsha 410208,China;College of Traditional Chinese Medicine,Hunan University of Chinese Medicine)

机构地区：[1]湖南中医药大学药学院,长沙410208 [2]湖南中医药大学中医学院

出　　处：《中国药师》2022年第8期1424-1430,共7页China Pharmacist

基　　金：湖南省卫生健康委科研重点课题(编号:202113052006);湖南省自科学科药联合基金项目(编号:2021JJ80012);湖南省药学一流学科开放基金项目(编号:2020YX01、2020YX07、2021YX12)。

摘　　要：蛋白降解靶向嵌合体(PROTAC)是能够通过泛素-蛋白酶体系对靶标蛋白直接起到降解作用的小分子化合物,其在小分子抑制药开发遭遇瓶颈时为药物开发提供了一种新的思路。PROTAC技术在抗肿瘤药物开发上的应用比较成熟,已经开发出多个用于降解肿瘤相关靶点的PROTAC分子。本文主要对这项技术在抗肿瘤药物开发中的进展及PROTAC分子修饰进行总结,为之后的PROTAC分子开发提供参考。Proteolysis targeting chimeria(PROTAC) is a small molecule compound that can directly degrade target proteins through the ubiquitin-protease system. The application of PROTAC technology in the development of anti-tumor drugs is relatively mature, and a number of PROTAC molecules have been developed for degrading tumor-related targets. This article mainly summarized the progress in this technology in the development of anti-tumor drugs and the modification of PROTAC molecules, so as to provide reference for the development of PROTAC molecules in the future.

关 键 词：蛋白降解靶向嵌合体 泛素-蛋白酶 肿瘤 分子修饰 

分 类 号：R914.2[医药卫生—药物化学]