1qcf: Difference between revisions
New page: left|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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[[Image:1qcf.gif|left|200px]]<br /> | [[Image:1qcf.gif|left|200px]]<br /><applet load="1qcf" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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caption="1qcf, resolution 2.0Å" /> | caption="1qcf, resolution 2.0Å" /> | ||
'''CRYSTAL STRUCTURE OF HCK IN COMPLEX WITH A SRC FAMILY-SELECTIVE TYROSINE KINASE INHIBITOR'''<br /> | '''CRYSTAL STRUCTURE OF HCK IN COMPLEX WITH A SRC FAMILY-SELECTIVE TYROSINE KINASE INHIBITOR'''<br /> | ||
==Overview== | ==Overview== | ||
The crystal structure of the autoinhibited form of Hck has been determined | 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== | ==About this Structure== | ||
1QCF is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with PP1 as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | 1QCF is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=PP1:'>PP1</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1QCF OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: tyrosine kinase-inhibitor complex]] | [[Category: tyrosine kinase-inhibitor complex]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:38:10 2008'' | ||
Revision as of 15:38, 21 February 2008
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CRYSTAL STRUCTURE OF HCK IN COMPLEX WITH A SRC FAMILY-SELECTIVE TYROSINE KINASE INHIBITOR
OverviewOverview
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 StructureAbout this Structure
1QCF is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
ReferenceReference
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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