摘要
蛋白水解靶向嵌合分子(protein proteolysis-targeting chimeras,PROTAC)是一种可以募集靶蛋白和靶蛋白降解酶的杂合双功能化合物,利用泛素-蛋白酶体途径特异性地降解靶蛋白。因为PROTAC有将无法成药的蛋白质作为靶蛋白的潜力以及可能在药物耐药中发挥作用的优势,近年来已赢得了广泛关注。本文总结了现有的PROTAC小分子在核蛋白、膜蛋白及胞浆蛋白等不同靶点研究中的应用。
The protein proteolysis-targeting chimeras(PROTAC)are a kind of bifunctional compound that can recruit target proteins and degrade the enzyme of target proteins.The mechanism of PROTAC is using the ubiquitin-proteasome pathway to degrade target protein specifically.Because of its potential to target non-proprietary proteins and to play roles in drug resistance,PROTAC has attracted wide attention.This review summarizes the application of small molecule PROTAC in previous studies of different targets,such as nuclear proteins,membrane proteins and cytoplasmic proteins.
作者
王媛
龙菁
唱祺
胡维稳
胡高云
李乾斌
WANG Yuan;LONG Jing;CHANG Qi;HU Wei-wen;HU Gao-yun;LI Qian-bin(Department of Medicinal Chemistry,Xiangya School of Pharmaceutical Sciences,Central South University,Changsha 410012,China;State Key Laboratory of Natural and Biomimetic Drugs,School of Pharmaceutical Sciences,Peking University,Beijing 100191,China;The Department of Dermatology,Xiangya Hospital,Central South University,Changsha 410012,China;Pharmaceutical Department,Yunnan Provincial Hospital of Traditional Chinese Medicine,Kunming 650021,China)
出处
《药学学报》
CAS
CSCD
北大核心
2020年第3期446-452,共7页
Acta Pharmaceutica Sinica
基金
国家自然科学基金资助项目(81803373,81573287,81773640).
关键词
PROTAC
耐药性
核蛋白
跨膜蛋白
胞浆蛋白
PROTAC
drug resistance
nuclear protein
membrane protein
cytoplasmic protein
作者简介
通讯作者:李乾斌,Tel:86-731-82650370,E-mail:qbli@csu.edu.cn
