Basic Information
ID: ALA5120797
Journal: J Med Chem
Title: Principles of Kinase Allosteric Inhibition and Pocket Validation.
Authors: Pan Y, Mader MM.
Abstract: With several marketed drugs, allosteric inhibition of kinases has translated to pharmacological effects and clinical benefits comparable to those from orthosteric inhibition. However, despite much effort over more than 20 years, the number of kinase targets associated with FDA-approved allosteric drugs is limited, suggesting the challenges in identifying and validating allosteric inhibitors. Here we review the principles of allosteric inhibition, summarize the discovery of allosteric MEK1/2 and BCR-ABL1 inhibitors, and discuss the approaches to screening and demonstrating the functional activity of allosteric pocket ligands.
CiteXplore: 35312319
DOI: 10.1021/acs.jmedchem.2c00073
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets