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Chembiochem. 2013 Nov 4;14(16):2119-25. doi: 10.1002/cbic.201300253. Epub 2013 Sep 12.

Allosteric lariat peptide inhibitors of Abl kinase.

Author information

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

Abstract

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.

KEYWORDS:

Abl kinase; combinatorial chemistry; enzyme inhibitors; lariat peptides; uncompetitive inhibition

PMID:
24030821
DOI:
10.1002/cbic.201300253
[Indexed for MEDLINE]
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