1gag

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[[Image:1gag.gif|left|200px]]
[[Image:1gag.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1gag |SIZE=350|CAPTION= <scene name='initialview01'>1gag</scene>, resolution 2.7&Aring;
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The line below this paragraph, containing "STRUCTURE_1gag", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=112:THIOPHOSPHORIC+ACID+O-((ADENOSYL-PHOSPHO)PHOSPHO)-S-ACETAMIDYL-DIESTER'>112</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|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>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_1gag| PDB=1gag | SCENE= }}
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|RELATEDENTRY=[[1ir3|1IR3]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1gag FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1gag OCA], [http://www.ebi.ac.uk/pdbsum/1gag PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1gag RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF THE INSULIN RECEPTOR KINASE IN COMPLEX WITH A BISUBSTRATE INHIBITOR'''
'''CRYSTAL STRUCTURE OF THE INSULIN RECEPTOR KINASE IN COMPLEX WITH A BISUBSTRATE INHIBITOR'''
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[[Category: Parang, K.]]
[[Category: Parang, K.]]
[[Category: Till, J H.]]
[[Category: Till, J H.]]
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[[Category: protein kinase inhibitor]]
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[[Category: Protein kinase inhibitor]]
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[[Category: tyrosine kinase]]
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[[Category: Tyrosine kinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 17:21:00 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:40:05 2008''
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Revision as of 14:21, 2 May 2008

Image:1gag.gif

Template:STRUCTURE 1gag

CRYSTAL STRUCTURE OF THE INSULIN RECEPTOR KINASE IN COMPLEX WITH A BISUBSTRATE INHIBITOR


Overview

Protein kinase inhibitors have applications as anticancer therapeutic agents and biological tools in cell signaling. Based on a phosphoryl transfer mechanism involving a dissociative transition state, a potent and selective bisubstrate inhibitor for the insulin receptor tyrosine kinase was synthesized by linking ATPgammaS to a peptide substrate analog via a two-carbon spacer. The compound was a high affinity competitive inhibitor against both nucleotide and peptide substrates and showed a slow off-rate. A crystal structure of this inhibitor bound to the tyrosine kinase domain of the insulin receptor confirmed the key design features inspired by a dissociative transition state, and revealed that the linker takes part in the octahedral coordination of an active site Mg2+. These studies suggest a general strategy for the development of selective protein kinase inhibitors.

About this Structure

1GAG is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Mechanism-based design of a protein kinase inhibitor., Parang K, Till JH, Ablooglu AJ, Kohanski RA, Hubbard SR, Cole PA, Nat Struct Biol. 2001 Jan;8(1):37-41. PMID:11135668 Page seeded by OCA on Fri May 2 17:21:00 2008

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