药物发现
共价键
药物开发
共价结合
化学
计算生物学
药品
食品药品监督管理局
药理学
生物化学
医学
生物
有机化学
作者
Avick Kumar Ghosh,Indranil Samanta,Anushree Mondal,Wenshe Ray Liu
出处
期刊:ChemMedChem
[Wiley]
日期:2019-03-26
卷期号:14 (9): 889-906
被引量:162
标识
DOI:10.1002/cmdc.201900107
摘要
Abstract Although covalent inhibitors have been used as therapeutics for more than a century, there has been general resistance in the pharmaceutical industry against their further development due to safety concerns. This inclination has recently been reverted after the development of a wide variety of covalent inhibitors to address human health conditions along with the US Food and Drug Administration (FDA) approval of several covalent therapeutics for use in humans. Along with this exciting resurrection of an old drug discovery concept, this review surveys enzymes that can be targeted by covalent inhibitors for the treatment of human diseases. We focus on protein kinases, RAS proteins, and a few other enzymes that have been studied extensively as targets for covalent inhibition, with the aim to address challenges in designing effective covalent drugs and to provide suggestions in the area that have yet to be explored.
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