1qcf

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{{STRUCTURE_1qcf| PDB=1qcf | SCENE= }}
{{STRUCTURE_1qcf| PDB=1qcf | SCENE= }}
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'''CRYSTAL STRUCTURE OF HCK IN COMPLEX WITH A SRC FAMILY-SELECTIVE TYROSINE KINASE INHIBITOR'''
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===CRYSTAL STRUCTURE OF HCK IN COMPLEX WITH A SRC FAMILY-SELECTIVE TYROSINE KINASE INHIBITOR===
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==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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(as it appears on PubMed at http://www.pubmed.gov), where 10360180 is the PubMed ID number.
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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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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 06:07:35 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 21:39:18 2008''

Revision as of 18:39, 27 July 2008

Image:1qcf.png

Template:STRUCTURE 1qcf

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

Template:ABSTRACT PUBMED 10360180

About this Structure

1QCF is a Single protein structure of sequence from Homo sapiens. 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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