1qcf: Difference between revisions
No edit summary |
No edit summary |
||
| Line 1: | Line 1: | ||
[[Image:1qcf.gif|left|200px]] | [[Image:1qcf.gif|left|200px]] | ||
<!-- | |||
The line below this paragraph, containing "STRUCTURE_1qcf", creates the "Structure Box" on the page. | |||
You may change the PDB parameter (which sets the PDB file loaded into the applet) | |||
or the SCENE parameter (which sets the initial scene displayed when the page is loaded), | |||
| | or leave the SCENE parameter empty for the default display. | ||
| | --> | ||
{{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''' | ||
| Line 31: | Line 28: | ||
[[Category: Schindler, T.]] | [[Category: Schindler, T.]] | ||
[[Category: Sicheri, F.]] | [[Category: Sicheri, F.]] | ||
[[Category: | [[Category: Down-regulated kinase]] | ||
[[Category: | [[Category: Ordered activation loop]] | ||
[[Category: | [[Category: Tyrosine kinase-inhibitor complex]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 06:07:35 2008'' | |||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | |||
Revision as of 06:07, 3 May 2008
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 Page seeded by OCA on Sat May 3 06:07:35 2008