共价修饰类药物的研究进展  

Advances of covalently modified drugs

作　　者：何思雨 孙昊鹏[1] 

机构地区：[1]中国药科大学药学院,南京211198

出　　处：《中国药科大学学报》2017年第5期503-514,共12页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.81573281)~~

摘　　要：共价修饰类药物通过共价键与靶标结合而发挥其药理作用,由于其可能带来脱靶效应及不良反应,长期以来在药物设计领域尽可能被避免。随着对已上市的重磅级共价药物结合模式的深入研究,越来越多共价修饰类药物重新得到研发人员的重视,寻找高选择性、低不良反应的共价修饰类药物已成为目前研究的热点。本文对一些共价修饰类药物进行分类,对其与靶标结合的模式以及近年来共价修饰类药物设计的新策略进行综述,为共价药物的合理药物设计提供参考。Covalently modified drugs,which exert their pharmacological effects by covalently binding to the targets,have been avoided as far as possible for a long time in drug design due to the potential off-target effects and other side-effects.With the in-depth study of binding modes of market blockbuster covalent drugs,more and more attention has been concentrated on covalently modified drugs.Current challenges remain in development of potent selective covalently modified drugs with fewer adverse effects.This paper reviews the classification of some covalently modified drugs,the drug-target binding modes and the new strategies of designing covalently modified drugs,in order to provide reference for rational design of covalent drugs.

关 键 词：共价修饰类药物 药物-靶标结合模式 合理药物设计 

分 类 号：R91[医药卫生—药学]