1gag: Difference between revisions

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[[Image:1gag.~~gif~~|left|200px]]

[[Image:1gag.png|left|200px]]

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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===

~~==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~~.

The line below this paragraph, {{ABSTRACT_PUBMED_11135668}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 11135668 is the PubMed ID number.

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==About this Structure==

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[[Category: Protein kinase inhibitor]]

[[Category: Tyrosine kinase]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Fri May~~ ~~2 17~~:21:00 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 04:59:36 2008''

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-[[Image:1gag.gif|left|200px]]
+{{Seed}}
+[[Image:1gag.png|left|200px]]
 <!--
@@ Line 9: / Line 10: @@
 {{STRUCTURE_1gag|  PDB=1gag  |  SCENE=  }}
-'''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===
-==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.
+The line below this paragraph, {{ABSTRACT_PUBMED_11135668}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 11135668 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_11135668}}
 ==About this Structure==
@@ Line 31: / Line 35: @@
 [[Category: Protein kinase inhibitor]]
 [[Category: Tyrosine kinase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May  2 17:21:00 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul  1 04:59:36 2008''