title: Allosteric lariat peptide inhibitors of Abl kinase.
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.
authors.affiliation: Department of Biochemistry, University of Saskatchewan, 107 Wiggins Road, Saskatoon, SK S7N 5E5 (Canada).
authors.forename: V M
authors.initials: VM
authors.lastname: Bharathikumar
authors.forename: Kris
authors.initials: K
authors.lastname: Barreto
authors.forename: John F
authors.initials: JF
authors.lastname: Decoteau
authors.forename: C Ronald
authors.initials: CR
authors.lastname: Geyer
mesh_terms: D000255:Adenosine Triphosphate / Q000737:chemistry / Q000378:metabolism; D000494:Allosteric Regulation; D000595:Amino Acid Sequence; D001665:Binding Sites; D020134:Catalytic Domain; D045744:Cell Line, Tumor; D004789:Enzyme Activation / Q000187:drug effects; D006801:Humans; D007700:Kinetics; D010455:Peptides / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D016315:Proto-Oncogene Proteins c-abl / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D010455:Peptides; D047428:Protein Kinase Inhibitors; D000255:Adenosine Triphosphate; D016315:Proto-Oncogene Proteins c-abl
keywords: Abl kinase; combinatorial chemistry; enzyme inhibitors; lariat peptides; uncompetitive inhibition