Allosteric lariat peptide inhibitors of Abl kinase.

CHEMBIOCHEM(2013)

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摘要
Going against tradition: although most kinase inhibitors are ATP competitive, lariat peptides inhibit Abl kinase activity in an ATP-uncompetitive manner. Further, lariat peptides discriminated Src family kinases, and recognize the allosteric region that lies adjacent to the ATP binding pocket in the Abl kinase catalytic cleft.
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关键词
Abl kinase,combinatorial chemistry,enzyme inhibitors,lariat peptides,uncompetitive inhibition
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