1gag

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[[Image:1gag.gif|left|200px]]
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{{STRUCTURE_1gag| PDB=1gag | SCENE= }}
{{STRUCTURE_1gag| PDB=1gag | SCENE= }}
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'''CRYSTAL STRUCTURE OF THE INSULIN RECEPTOR KINASE IN COMPLEX WITH A BISUBSTRATE INHIBITOR'''
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===CRYSTAL STRUCTURE OF THE INSULIN RECEPTOR KINASE IN COMPLEX WITH A BISUBSTRATE INHIBITOR===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 11135668 is the PubMed ID number.
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{{ABSTRACT_PUBMED_11135668}}
==About this Structure==
==About this Structure==
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[[Category: Protein kinase inhibitor]]
[[Category: Protein kinase inhibitor]]
[[Category: Tyrosine kinase]]
[[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 Tue Jul 1 04:59:36 2008''

Revision as of 01:59, 1 July 2008

Image:1gag.png

Template:STRUCTURE 1gag

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

Template:ABSTRACT PUBMED 11135668

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

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