Covalent Small Molecules as Enabling Platforms for Drug Discovery

被引：69

作者：

Dalton, Samuel E. ^{[1
]}

Campos, Sebastien ^{[2
]}

机构：

[1] Astex Pharmaceut, 436 Cambridge Sci Pk,Milton Rd, Cambridge CB4 0QA, England

[2] Pharmaron, Drug Discovery Serv Europe, Hertford Rd, Hoddesdon EN11 9BU, Herts, England

来源：

CHEMBIOCHEM | 2020年 / 21卷 / 08期

关键词：

ABPP; covalent; fragments; photoaffinity; PROTAC; TARGETED PROTEIN-DEGRADATION; CHEMICAL-GENETIC APPROACH; SELECTIVE INHIBITORS; IRREVERSIBLE INHIBITOR; SULFONYL FLUORIDES; WIDE SELECTIVITY; UBIQUITIN LIGASE; FAAH INHIBITOR; REACTIVE GROUP; IN-VIVO;

D O I：

10.1002/cbic.201900674

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：1080 / 1100

页数：21

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