Perturbation of biological processes with small molecule kinase inhibitors

Wenyang Li; Jue Wang; Ruqi Liang; Xiaoguang Lei

doi:10.1016/j.cbpa.2022.102185

Perturbation of biological processes with small molecule kinase inhibitors

Curr Opin Chem Biol. 2022 Oct:70:102185. doi: 10.1016/j.cbpa.2022.102185. Epub 2022 Jul 16.

Authors

Wenyang Li¹, Jue Wang¹, Ruqi Liang², Xiaoguang Lei³

Affiliations

¹ Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Department of Chemical Biology, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
² Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Department of Chemical Biology, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China; Academy for Advanced Interdisciplinary Studies, Peking University, Beijing 100871, China; Peking-Tsinghua Center for Life Sciences, Peking University, Beijing 100871, China.
³ Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Department of Chemical Biology, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China; Academy for Advanced Interdisciplinary Studies, Peking University, Beijing 100871, China; Peking-Tsinghua Center for Life Sciences, Peking University, Beijing 100871, China; Institute for Cancer Research, Shenzhen Bay Laboratory, Shenzhen, China. Electronic address: xglei@pku.edu.cn.

PMID: 35853282
DOI: 10.1016/j.cbpa.2022.102185

Abstract

The reversible phosphorylation of substrates mediated by kinases and phosphatases affects their subcellular localization, catalytic activity, and/or interaction with other molecules. It is essential for signal transduction and the regulation of nearly all cellular processes, such as proliferation, apoptosis, metabolism, motility, and differentiation. Small molecule kinase inhibitors (SMKIs) have served as critical chemical probes to reveal the biological functions and mechanisms of kinases and their potential as therapeutic targets. In this review, we focused on a few novel SMKIs and their recent application in biological and preclinical studies to showcase how highly selective and potent SMKIs can be developed and utilized to propel the investigations on kinases and the biology behind.

Keywords: Cancer; Chemical genetics; Chemical probes; Drug discovery; Small molecule kinase inhibitors (SMKIs).

Publication types

Review

MeSH terms

Biological Phenomena*
Phosphoric Monoester Hydrolases
Phosphorylation
Protein Kinase Inhibitors* / therapeutic use
Signal Transduction / physiology

Substances

Protein Kinase Inhibitors
Phosphoric Monoester Hydrolases