The ins and outs of selective kinase inhibitor development

October 20th, 2015 by Susanne Müller

Nature Chemical Biology 11, 818 (2015). doi:10.1038/nchembio.1938

Authors: Susanne Müller, Apirat Chaikuad, Nathanael S Gray & Stefan Knapp

Protein kinases have emerged as one of the most successful families of drug targets. To date, most selective kinase inhibitors have been discovered serendipitously either through broad selectivity screening or through the discovery of unique binding modes. Here we discuss design strategies that could lead to a broader coverage of the kinome with selective inhibitors and to a more rational approach for developing them.