1qcf: Difference between revisions

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{{STRUCTURE_1qcf|  PDB=1qcf  |  SCENE=  }}  
{{STRUCTURE_1qcf|  PDB=1qcf  |  SCENE=  }}  


'''CRYSTAL STRUCTURE OF HCK IN COMPLEX WITH A SRC FAMILY-SELECTIVE TYROSINE KINASE INHIBITOR'''
===CRYSTAL STRUCTURE OF HCK IN COMPLEX WITH A SRC FAMILY-SELECTIVE TYROSINE KINASE INHIBITOR===




==Overview==
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The crystal structure of the autoinhibited form of Hck has been determined at 2.0 A resolution, in complex with a specific pyrazolo pyrimidine-type inhibitor, PP1. The activation segment, a key regulatory component of the catalytic domain, is unphosphorylated and is visualized in its entirety. Tyr-416, the site of activating autophosphorylation in the Src family kinases, is positioned such that access to the catalytic machinery is blocked. PP1 is bound at the ATP-binding site of the kinase, and a methylphenyl group on PP1 is inserted into an adjacent hydrophobic pocket. The enlargement of this pocket in autoinhibited Src kinases suggests a route toward the development of inhibitors that are specific for the inactive forms of these proteins.
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{{ABSTRACT_PUBMED_10360180}}


==About this Structure==
==About this Structure==
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[[Category: Ordered activation loop]]
[[Category: Ordered activation loop]]
[[Category: Tyrosine kinase-inhibitor complex]]
[[Category: Tyrosine kinase-inhibitor complex]]
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