1qcf: Difference between revisions
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|PDB= 1qcf |SIZE=350|CAPTION= <scene name='initialview01'>1qcf</scene>, resolution 2.0Å | |PDB= 1qcf |SIZE=350|CAPTION= <scene name='initialview01'>1qcf</scene>, resolution 2.0Å | ||
|SITE= | |SITE= | ||
|LIGAND= <scene name='pdbligand=PP1:1-TER-BUTYL-3-P-TOLYL-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLAMINE'>PP1</scene> | |LIGAND= <scene name='pdbligand=PP1:1-TER-BUTYL-3-P-TOLYL-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-YLAMINE'>PP1</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene> | ||
|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
|DOMAIN= | |||
|RELATEDENTRY=[[1ad5|1AD5]] | |||
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1qcf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1qcf OCA], [http://www.ebi.ac.uk/pdbsum/1qcf PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1qcf RCSB]</span> | |||
}} | }} | ||
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[[Category: Schindler, T.]] | [[Category: Schindler, T.]] | ||
[[Category: Sicheri, F.]] | [[Category: Sicheri, F.]] | ||
[[Category: down-regulated kinase]] | [[Category: down-regulated kinase]] | ||
[[Category: ordered activation loop]] | [[Category: ordered activation loop]] | ||
[[Category: tyrosine kinase-inhibitor complex]] | [[Category: tyrosine kinase-inhibitor complex]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:11:46 2008'' | ||
Revision as of 23:11, 30 March 2008
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| , resolution 2.0Å | |||||||
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| Ligands: | , | ||||||
| Related: | 1AD5
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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. 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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