靶向共价键药物的研究进展

Research Progress of Targeted Covalent Drugs

药物与靶标的结合是启动药理作用的本源,共价键药物是以共享电子的方式来实现与靶标的结合,其中大多为抗感染、抗肿瘤以及心脑血管、神经系统和代谢类药物。简介共价键药物与非共价键药物的区别以及既往的重磅级共价键药物与靶标的结合特点,分类综述靶向共价键药物的理性设计及与靶标的结合反应。

Pharmacological effects origilmte from tile interactions of drugs with targets. The covalent bindings of drugs to targets are achievedby sharing electron pairs, which have been tbund mostly in the interactions of the drugs for infction, tumor and the central nervous system, cardio-cerebrovascular and metabolic diseases with their targets. The distinction between covalent drug and non-covalent drug and tile binding tbatures of the launched heavyweight covalent drugs to their targets were introduced. The rational design of covalent drugs and their binding reactions withtheir targets were reviewed classifiedly.