Issue 7, 2022

Reactivity-based chemical-genetic study of protein kinases

Abstract

The human protein kinase superfamily comprises over 500 members that operate in nearly every signal transduction pathway and regulate essential cellular processes. Deciphering the functional roles of protein kinases with small-molecule inhibitors is essential to enhance our understanding of cell signaling and to facilitate the development of new therapies. However, it is rather challenging to identify selective kinase inhibitors because of the conserved nature of the ATP binding site. A number of chemical-genetic approaches have been developed during the past two decades to enable selective chemical perturbation of the activity of individual kinases. Herein, we review the development and application of chemical-genetic strategies that feature the use of covalent inhibitors targeting cysteine residues to dissect the cellular functions of protein kinases.

Graphical abstract: Reactivity-based chemical-genetic study of protein kinases

Article information

Article type
Review Article
Submitted
17 dec 2021
Accepted
28 mrt 2022
First published
30 mrt 2022

RSC Med. Chem., 2022,13, 783-797

Author version available

Reactivity-based chemical-genetic study of protein kinases

R. Rezende Miranda and C. Zhang, RSC Med. Chem., 2022, 13, 783 DOI: 10.1039/D1MD00389E

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