The ins and outs of selective kinase inhibitor development

The ins and outs of selective kinase inhibitor development

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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. Access through your institution Buy or subscribe This is a preview of subscription content, access via your institution ACCESS OPTIONS Access


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Susanne Müller and Apirat Chaikuad are at the Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Oxford, UK., Susanne Müller & Apirat


Chaikuad * Nathanael S. Gray is at the Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA., Nathanael S Gray * Stefan Knapp is at the


Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Oxford, UK and the Institute for Pharmaceutical Chemistry and Buchmann Institute for Molecular


Life Sciences, Johann Wolfgang Goethe-University, Frankurt am Main, Germany., Stefan Knapp Authors * Susanne Müller View author publications You can also search for this author inPubMed 


Google Scholar * Apirat Chaikuad View author publications You can also search for this author inPubMed Google Scholar * Nathanael S Gray View author publications You can also search for this


author inPubMed Google Scholar * Stefan Knapp View author publications You can also search for this author inPubMed Google Scholar CORRESPONDING AUTHORS Correspondence to Nathanael S Gray


or Stefan Knapp. ETHICS DECLARATIONS COMPETING INTERESTS The authors declare no competing financial interests. RIGHTS AND PERMISSIONS Reprints and permissions ABOUT THIS ARTICLE CITE THIS


ARTICLE Müller, S., Chaikuad, A., Gray, N. _et al._ The ins and outs of selective kinase inhibitor development. _Nat Chem Biol_ 11, 818–821 (2015). https://doi.org/10.1038/nchembio.1938


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