Controlling the Covalent Reactivity of a Kinase Inhibitor with Light
Abstract
Covalent kinase inhibitors account for some of the most successful drugs that have recently entered the clinic and many others are in preclinical development. A common strategy is to target cysteines in the vicinity of the ATP binding site using an acrylamide electrophile. To increase the tissue selectivity of kinase inhibitors, it could be advantageous to control the reactivity of these electrophiles with light. Here, we introduce covalent...
Paper Details
Title
Controlling the Covalent Reactivity of a Kinase Inhibitor with Light
Published Date
Aug 11, 2021
Journal
Volume
60
Issue
37
Pages
20178 - 20183
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