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靶向共价键药物的研究进展
引用本文:郭宗儒.靶向共价键药物的研究进展[J].药学进展,2013(11):555-564.
作者姓名:郭宗儒
作者单位:中国医学科学院北京协和医学院药物研究所,北京100050
摘    要: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。

关 键 词:共价键药物  药物理性设计  药物-靶标结合反应

Research Progress of Targeted Covalent Drugs
GUO Zongru.Research Progress of Targeted Covalent Drugs[J].Progress in Pharmaceutical Sciences,2013(11):555-564.
Authors:GUO Zongru
Institution:GUO Zongru (Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing lO0050,China)
Abstract: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.
Keywords:covalent drug  rational drug design  drug-target binding reaction
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