1qcf
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(New page: 200px<br /> <applet load="1qcf" size="450" color="white" frame="true" align="right" spinBox="true" caption="1qcf, resolution 2.0Å" /> '''CRYSTAL STRUCTURE OF...)
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Revision as of 16:45, 12 November 2007
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CRYSTAL STRUCTURE OF HCK IN COMPLEX WITH A SRC FAMILY-SELECTIVE TYROSINE KINASE INHIBITOR
Overview
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.
About this Structure
1QCF is a Single protein structure of sequence from Homo sapiens with PP1 as ligand. Full crystallographic information is available from OCA.
Reference
Crystal structure of Hck in complex with a Src family-selective tyrosine kinase inhibitor., Schindler T, Sicheri F, Pico A, Gazit A, Levitzki A, Kuriyan J, Mol Cell. 1999 May;3(5):639-48. PMID:10360180
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