The presence of 491 very similar protein kinases in humans has proven to be a serious obstacle to generating specific kinase inhibitors and assessing their selectivity. Now, rational drug design has led to the generation of an irreversible kinase inhibitor with built-in features for demonstrating specificity in cells.
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Frödin, M. A RSK kinase inhibitor reporting its selectivity in vivo. Nat Chem Biol 3, 138–139 (2007). https://doi.org/10.1038/nchembio0307-138
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DOI: https://doi.org/10.1038/nchembio0307-138
