1y57
From Proteopedia
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|PDB= 1y57 |SIZE=350|CAPTION= <scene name='initialview01'>1y57</scene>, resolution 1.91Å | |PDB= 1y57 |SIZE=350|CAPTION= <scene name='initialview01'>1y57</scene>, resolution 1.91Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= | + | |LIGAND= <scene name='pdbligand=MPZ:4-[(4-METHYLPIPERAZIN-1-YL)METHYL]-N-{3-[(4-PYRIDIN-3-YLPYRIMIDIN-2-YL)AMINO]PHENYL}BENZAMIDE'>MPZ</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> |
| - | |ACTIVITY= [http://en.wikipedia.org/wiki/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 and 2.7.10.2 2.7.10.1 and 2.7.10.2] | + | |ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Transferase Transferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 and 2.7.10.2 2.7.10.1 and 2.7.10.2] </span> |
|GENE= SRC ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= SRC ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[2src|2SRC]], [[1fmk|1FMK]], [[1ksw|1KSW]], [[2ptk|2PTK]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1y57 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1y57 OCA], [http://www.ebi.ac.uk/pdbsum/1y57 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1y57 RCSB]</span> | ||
}} | }} | ||
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[[Category: Manley, P W.]] | [[Category: Manley, P W.]] | ||
[[Category: Meyer, T.]] | [[Category: Meyer, T.]] | ||
| - | [[Category: MPZ]] | ||
| - | [[Category: SO4]] | ||
[[Category: kinase structure]] | [[Category: kinase structure]] | ||
[[Category: sh2]] | [[Category: sh2]] | ||
[[Category: sh3]] | [[Category: sh3]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:58:58 2008'' |
Revision as of 21:59, 30 March 2008
| |||||||
| , resolution 1.91Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , | ||||||
| Gene: | SRC (Homo sapiens) | ||||||
| Activity: | Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2 | ||||||
| Related: | 2SRC, 1FMK, 1KSW, 2PTK
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Structure of unphosphorylated c-Src in complex with an inhibitor
Contents |
Overview
The regulation of the activity of Abl and Src family tyrosine kinases is mediated by intramolecular interactions between the SH3, SH2, and kinase (SH1) domains. We have determined the crystal structure of an unphosphorylated form of c-Src in which the SH2 domain is not bound to the C-terminal tail. This results in an open structure where the kinase domain adopts an active conformation and the C terminus binds within a hydrophobic pocket in the C-terminal lobe. NMR binding studies support the hypothesis that an N-terminal myristate could bind in this pocket, as observed for Abl, suggesting that c-Src may also be regulated by myristate binding. In addition, the structure contains a des-methyl analog of the antileukemia drug imatinib (STI571; Gleevec). This structure reveals why the drug shows a low affinity for active kinase conformations, contributing to its excellent kinase selectivity profile.
Disease
Known disease associated with this structure: Colon cancer, advanced OMIM:[190090]
About this Structure
1Y57 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation., Cowan-Jacob SW, Fendrich G, Manley PW, Jahnke W, Fabbro D, Liebetanz J, Meyer T, Structure. 2005 Jun;13(6):861-71. PMID:15939018
Page seeded by OCA on Mon Mar 31 00:58:58 2008
Categories: Homo sapiens | Single protein | Transferase | Cowan-Jacob, S W. | Fabbro, D. | Fendrich, G. | Jahnke, W. | Liebetanz, J. | Manley, P W. | Meyer, T. | Kinase structure | Sh2 | Sh3
