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Allosteric Lariat Peptide Inhibitors of Abl Kinase
Author(s) -
Bharathikumar V. M.,
Barreto Kris,
DeCoteau John F.,
Geyer C. Ronald
Publication year - 2013
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201300253
Subject(s) - allosteric regulation , kinase , abl , biochemistry , enzyme , chemistry , allosteric enzyme , proto oncogene tyrosine protein kinase src , peptide , protein kinase a , tyrosine kinase , receptor
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.