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The ins and outs of selective kinase inhibitor development

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.

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Figure 1: Milestones in kinase drug and inhibitor discovery.
Figure 2: Canonical kinase inhibitor binding modes and examples of selective inhibitors.

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Correspondence to Nathanael S Gray or Stefan Knapp.

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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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