title: Backbone assignment of the tyrosine kinase Src catalytic domain in complex with imatinib.
abstract: The Src tyrosine kinase is the paradigm of an oncogenic kinase, and of regulation by intramolecular inhibitory interactions, as well as an important anticancer target due to its roles in cell proliferation and metastasis. The assignment of backbone (1)H(N), (13)C(α), (13)CO, and (15)N, and sidechain (13)C(β) resonances of the catalytic domain of Src (283 residues) in complex with the anticancer drug Imatinib is reported here. Consistent with previous X-ray studies of the same complex, most signals from the activation loop are not detected, indicating that, even in the presence of the drug, it probably adopts highly heterogeneous conformations in intermediate exchange. For the rest of the polypeptide backbone, assignments have been completed for ~88% of residues, with only a few solvent-exposed amides remaining unassigned.
authors.affiliation: Spectroscopy and NMR Unit, Structural and Computational Biology Programme, Spanish National Cancer Center (CNIO), C. Melchor Fernández Almagro, 3, 28029, Madrid, Spain. rcampos@cnio.es
authors.forename: Ramón
authors.initials: R
authors.lastname: Campos-Olivas
authors.forename: Marco
authors.initials: M
authors.lastname: Marenchino
authors.forename: Leonardo
authors.initials: L
authors.lastname: Scapozza
authors.forename: Francesco L
authors.initials: FL
authors.lastname: Gervasio
mesh_terms: D000818:Animals; D001549:Benzamides; D020134:Catalytic Domain; D002645:Chickens; D000068877:Imatinib Mesylate; D019906:Nuclear Magnetic Resonance, Biomolecular; D010879:Piperazines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D011743:Pyrimidines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D011994:Recombinant Proteins / Q000737:chemistry / Q000378:metabolism; D018909:src Homology Domains; D019061:src-Family Kinases / Q000737:chemistry* / Q000378:metabolism
chemical_list: D001549:Benzamides; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D011994:Recombinant Proteins; D000068877:Imatinib Mesylate; D019061:src-Family Kinases