Magic bullets for protein kinases.

  title={Magic bullets for protein kinases.},
  author={Anthony C. Bishop and Oleksandr V. Buzko and Kevan M. Shokat},
  journal={Trends in cell biology},
  volume={11 4},
A chemical-genetic method for the generation of target-specific protein kinase inhibitors has been developed recently. This strategy utilizes a functionally silent active-site mutation to sensitize a target kinase to inhibition by a small molecule that does not inhibit wild-type kinases. Tyrosine and serine/threonine kinases are equally amenable to the drug-sensitization approach, which has been used to generate selective inhibitors of mutant Src-family kinases, Abl-family kinases, cyclin… CONTINUE READING

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