3c1x: Difference between revisions

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[[Image:3c1x.~~jpg~~|left|200px]]

[[Image:3c1x.png|left|200px]]

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~~'''~~Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-MET in complex with a Pyrrolotriazine based inhibitor~~'''~~

===Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-MET in complex with a Pyrrolotriazine based inhibitor===

~~==Overview==~~

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~~An amide library derived from the pyrrolo[2,1-f][1~~,2,~~4]triazine scaffold led~~ to the ~~identification of modest inhibitors of Met kinase activity~~. ~~Introduction of polar side chains at C-6 of the pyrrolotriazine core provided significant improvements in in vitro potency~~. ~~The amide moiety could be replaced with acylurea and malonamide substituents to give compounds with improved potency in~~ the ~~Met-driven GTL-16 human gastric carcinoma cell line~~. ~~Acylurea pyrrolotriazines with substitution at C-5 demonstrated single digit nanomolar kinase activity. X~~-~~ray crystallography revealed that the C~~-~~5 substituted pyrrolotriazines bind to the Met kinase domain in an ATP-competitive manner.~~

The line below this paragraph, {{ABSTRACT_PUBMED_18289854}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 18289854 is the PubMed ID number.

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==Disease==

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[[Category: Transmembrane]]

[[Category: Tyrosine-protein kinase]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sun May 4 21~~:17:44 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:11:35 2008''

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-[[Image:3c1x.jpg|left|200px]]
+{{Seed}}
+[[Image:3c1x.png|left|200px]]
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 {{STRUCTURE_3c1x|  PDB=3c1x  |  SCENE=  }}
-'''Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-MET in complex with a Pyrrolotriazine based inhibitor'''
+===Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-MET in complex with a Pyrrolotriazine based inhibitor===
-==Overview==
+<!--
-An amide library derived from the pyrrolo[2,1-f][1,2,4]triazine scaffold led to the identification of modest inhibitors of Met kinase activity. Introduction of polar side chains at C-6 of the pyrrolotriazine core provided significant improvements in in vitro potency. The amide moiety could be replaced with acylurea and malonamide substituents to give compounds with improved potency in the Met-driven GTL-16 human gastric carcinoma cell line. Acylurea pyrrolotriazines with substitution at C-5 demonstrated single digit nanomolar kinase activity. X-ray crystallography revealed that the C-5 substituted pyrrolotriazines bind to the Met kinase domain in an ATP-competitive manner.
+The line below this paragraph, {{ABSTRACT_PUBMED_18289854}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 18289854 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_18289854}}
 ==Disease==
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 [[Category: Transmembrane]]
 [[Category: Tyrosine-protein kinase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 21:17:44 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:11:35 2008''