1yoj: Difference between revisions
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'''Crystal structure of Src kinase domain''' | '''Crystal structure of Src kinase domain''' | ||
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[[Category: Schaefer, W.]] | [[Category: Schaefer, W.]] | ||
[[Category: Scheiblich, S.]] | [[Category: Scheiblich, S.]] | ||
[[Category: | [[Category: Protein tyrosine kinase]] | ||
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Revision as of 16:35, 3 May 2008
Crystal structure of Src kinase domain
OverviewOverview
c-Src was the first proto-oncoprotein to be identified, and has become the focus of many drug discovery programs. Src structures of a major inactive form have shown how the protein kinase is rigidified by several interdomain interactions; active configurations of Src are generated by release from this "assembled" or "bundled" form. Despite the importance of Src as a drug target, there is relatively little structural information available regarding the presumably more flexible active forms. Here we report three crystal structures of a dimeric active c-Src kinase domain, in an apo and two ligand complexed forms, with resolutions ranging from 2.9A to 1.95A. The structures show how the kinase domain, in the absence of the rigidifying interdomain interactions of the inactivation state, adopts a more open and flexible conformation. The ATP site inhibitor CGP77675 binds to the protein kinase with canonical hinge hydrogen bonds and also to the c-Src specific threonine 340. In contrast to purvalanol B binding in CDK2, purvalanol A binds in c-Src with a conformational change in a more open ATP pocket.
About this StructureAbout this Structure
1YOJ is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
Crystal structures of active SRC kinase domain complexes., Breitenlechner CB, Kairies NA, Honold K, Scheiblich S, Koll H, Greiter E, Koch S, Schafer W, Huber R, Engh RA, J Mol Biol. 2005 Oct 21;353(2):222-31. PMID:16168436 Page seeded by OCA on Sat May 3 16:35:11 2008