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Covalent inhibitors: a rational approach to drug discovery
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-07-02 , DOI: 10.1039/d0md00154f
Fandi Sutanto 1 , Markella Konstantinidou 1 , Alexander Dömling 1
Affiliation  

Covalent inhibitors are recognized as an important component in drug discovery and therapeutics. Since the first appearance of covalent inhibitors in the late 18th century, the field has advanced significantly and currently about 30% of the marketed drugs are covalent inhibitors. The numerous advantages of covalent inhibitors are counteracting the initial concerns regarding potential off-target toxicity. Thus, continuous research, especially for cancer targets is reported. The aim of this review is to provide a short historic overview and focus on recently developed covalent inhibitors (2011–2019), including structural aspects and examples on challenging targets.

中文翻译:


共价抑制剂:药物发现的合理方法



共价抑制剂被认为是药物发现和治疗的重要组成部分。自 18 世纪末共价抑制剂首次出现以来,该领域取得了显着进展,目前约 30% 的上市药物是共价抑制剂。共价抑制剂的众多优点抵消了最初对潜在脱靶毒性的担忧。因此,不断进行研究,特别是针对癌症靶点的研究。本综述的目的是提供简短的历史概述,并重点关注最近开发的共价抑制剂(2011-2019),包括结构方面和具有挑战性的目标的示例。
更新日期:2020-08-20
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