Covalent Small Molecules as Enabling Platforms for Drug Discovery.,ChemBioChem

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Covalent Small Molecules as Enabling Platforms for Drug Discovery.
ChemBioChem ( IF 2.6 ) Pub Date : 2020-02-04 , DOI: 10.1002/cbic.201900674
Samuel E Dalton ₁ , Sebastien Campos ₂

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Covalent drugs have experienced significant renewed interest in drug discovery. This resurgence has been accompanied by a better understanding of the reactivity relationships required to engage selective covalent bonds between nucleophilic proteins and electrophilic small molecules. As a result, researchers have come to the realisation that covalent molecules could also represent useful and novel tools aimed at supporting medicinal chemistry programmes. This review surveys the increasing number of drug discovery platforms employing covalent chemistries, and highlights the utility of these techniques for identifying and characterising small molecules and biological targets.

中文翻译：

共价小分子作为药物发现的支持平台。

共价药物在药物发现方面经历了重大的重新关注。这种回潮伴随着对亲核蛋白和亲电子小分子之间选择性共价键结合所需反应性关系的更好理解。结果，研究人员已经意识到共价分子也可以代表旨在支持药物化学程序的有用且新颖的工具。这篇综述调查了采用共价化学方法的药物发现平台的数量不断增加的情况，并着重介绍了这些技术在鉴定和表征小分子和生物学靶标方面的实用性。

更新日期：2020-02-04

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