Allosteric Lariat Peptide Inhibitors of Abl Kinase

Authors

  • V. M. Bharathikumar,

    1. Department of Biochemistry, University of Saskatchewan, 107 Wiggins Road, Saskatoon, SK S7N 5E5 (Canada)
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  • Dr. Kris Barreto,

    1. Department of Biochemistry, University of Saskatchewan, 107 Wiggins Road, Saskatoon, SK S7N 5E5 (Canada)
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  • Prof. John F. DeCoteau,

    1. Department of Pathology, University of Saskatchewan, 103 Hospital Drive, Saskatoon, SK S7N 0W8 (Canada)
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  • Prof. C. Ronald Geyer

    Corresponding author
    1. Department of Biochemistry, University of Saskatchewan, 107 Wiggins Road, Saskatoon, SK S7N 5E5 (Canada)
    • Department of Biochemistry, University of Saskatchewan, 107 Wiggins Road, Saskatoon, SK S7N 5E5 (Canada)

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Abstract

original image

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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