3bu5: Difference between revisions

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Revision as of 20:01, 20 March 2008

File:3bu5.jpg

, resolution 2.10Å

Sites:

and

Ligands:

and

Gene:

INSR (Homo sapiens)

Activity:

Receptor protein-tyrosine kinase, with EC number 2.7.10.1

Coordinates:

save as pdb, mmCIF, xml

Crystal structure of the insulin receptor kinase in complex with IRS2 KRLB peptide and ATP

OverviewOverview

Insulin receptor substrates 1 and 2 (IRS1 and -2) are crucial adaptor proteins in mediating the metabolic and mitogenic effects of insulin and insulin-like growth factor 1. These proteins consist of a pleckstrin homology domain, a phosphotyrosine binding domain and a C-terminal region containing numerous sites of tyrosine, serine and threonine phosphorylation. Previous yeast two-hybrid studies identified a region unique to IRS2, termed the kinase regulatory-loop binding (KRLB) region, which interacts with the tyrosine kinase domain of the insulin receptor. Here we present the crystal structure of the insulin receptor kinase in complex with a 15-residue peptide from the KRLB region. In the structure, this segment of IRS2 is bound in the kinase active site with Tyr628 positioned for phosphorylation. Although Tyr628 was phosphorylated by the insulin receptor, its catalytic turnover was poor, resulting in kinase inhibition. Our studies indicate that the KRLB region functions to limit tyrosine phosphorylation of IRS2.

About this StructureAbout this Structure

3BU5 is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

Structural and biochemical characterization of the KRLB region in insulin receptor substrate-2., Wu J, Tseng YD, Xu CF, Neubert TA, White MF, Hubbard SR, Nat Struct Mol Biol. 2008 Mar;15(3):251-8. Epub 2008 Feb 17. PMID:18278056

Page seeded by OCA on Thu Mar 20 19:01:18 2008

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

@@ Line 1: / Line 1: @@
-[[Image:3bu5.jpg|left|200px]]<br /><applet load="3bu5" size="350" color="white" frame="true" align="right" spinBox="true"
+[[Image:3bu5.jpg|left|200px]]
-caption="3bu5, resolution 2.10&Aring;" />
-'''Crystal structure of the insulin receptor kinase in complex with IRS2 KRLB peptide and ATP'''<br />
+ {{Structure
+|PDB= 3bu5 |SIZE=350|CAPTION= <scene name='initialview01'>3bu5</scene>, resolution 2.10&Aring;
+|SITE= <scene name='pdbsite=AC1:Mg+Binding+Site+For+Residue+A+301'>AC1</scene> and <scene name='pdbsite=AC2:Atp+Binding+Site+For+Residue+A+300'>AC2</scene>
+|LIGAND= <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene> and <scene name='pdbligand=ATP:ADENOSINE-5'-TRIPHOSPHATE'>ATP</scene>
+|ACTIVITY= [http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1]
+|GENE= INSR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+}}
+'''Crystal structure of the insulin receptor kinase in complex with IRS2 KRLB peptide and ATP'''
 ==Overview==
@@ Line 7: / Line 16: @@
 ==About this Structure==
-BU5 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=MG:'>MG</scene> and <scene name='pdbligand=ATP:'>ATP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Receptor_protein-tyrosine_kinase Receptor protein-tyrosine kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.10.1 2.7.10.1] Known structural/functional Sites: <scene name='pdbsite=AC1:Mg+Binding+Site+For+Residue+A+301'>AC1</scene> and <scene name='pdbsite=AC2:Atp+Binding+Site+For+Residue+A+300'>AC2</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3BU5 OCA].
+BU5 is a [[Protein complex]] structure of sequences 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=3BU5 OCA].
 ==Reference==
-Structural and biochemical characterization of the KRLB region in insulin receptor substrate-2., Wu J, Tseng YD, Xu CF, Neubert TA, White MF, Hubbard SR, Nat Struct Mol Biol. 2008 Mar;15(3):251-8. Epub 2008 Feb 17. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=18278056 18278056]
+Structural and biochemical characterization of the KRLB region in insulin receptor substrate-2., Wu J, Tseng YD, Xu CF, Neubert TA, White MF, Hubbard SR, Nat Struct Mol Biol. 2008 Mar;15(3):251-8. Epub 2008 Feb 17. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/18278056 18278056]
 [[Category: Homo sapiens]]
 [[Category: Protein complex]]
@@ Line 42: / Line 51: @@
 [[Category: tyrosine-protein kinase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Mar 14 09:44:12 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 19:01:18 2008''