CHAPTER 8: Chemical Probes for Kinases Check Access
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Published:17 Nov 2020
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Special Collection: 2020 ebook collectionSeries: Chemical Biology
X. Lu, J. B. Smaill, and K. Ding, in The Discovery and Utility of Chemical Probes in Target Discovery, ed. P. Brennan and S. V. Rodriguez, The Royal Society of Chemistry, 2020, pp. 182-213.
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Chemical probes that function through inhibition of kinase signalling represent a promising approach for the discovery of targeted therapeutics. The majority of developed kinase chemical probes are characterized as ATP competitive (type I and II), allosteric (type III and IV) and irreversible inhibitors. This chapter reviews representative chemical probes for some kinases and highlights the unique binding modes for each type. Additionally, chemical probes with new binding modes, including binding to the extracellular domain and proteolysis-targeting chimeras (PROTACs), are also addressed.