1y57

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[[Image:1y57.gif|left|200px]]<br /><applet load="1y57" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1y57.gif|left|200px]]
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caption="1y57, resolution 1.91&Aring;" />
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'''Structure of unphosphorylated c-Src in complex with an inhibitor'''<br />
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{{Structure
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|PDB= 1y57 |SIZE=350|CAPTION= <scene name='initialview01'>1y57</scene>, resolution 1.91&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene> and <scene name='pdbligand=MPZ:4-[(4-METHYLPIPERAZIN-1-YL)METHYL]-N-{3-[(4-PYRIDIN-3-YLPYRIMIDIN-2-YL)AMINO]PHENYL}BENZAMIDE'>MPZ</scene>
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|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]
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|GENE= SRC ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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}}
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'''Structure of unphosphorylated c-Src in complex with an inhibitor'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1Y57 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=SO4:'>SO4</scene> and <scene name='pdbligand=MPZ:'>MPZ</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1Y57 OCA].
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1Y57 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1Y57 OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15939018 15939018]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/15939018 15939018]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: sh3]]
[[Category: sh3]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:01:58 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:18:34 2008''

Revision as of 13:18, 20 March 2008

Image:1y57.gif


PDB ID 1y57

Drag the structure with the mouse to rotate
, resolution 1.91Å
Ligands: and
Gene: SRC (Homo sapiens)
Activity: Transferase, with EC number and 2.7.10.2 2.7.10.1 and 2.7.10.2
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

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