2ghm: Difference between revisions

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[[Image:2ghm.gif|left|200px]]
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{{STRUCTURE_2ghm|  PDB=2ghm  |  SCENE=  }}  
{{STRUCTURE_2ghm|  PDB=2ghm  |  SCENE=  }}  


'''Mutated MAP kinase P38 (Mus Musculus) in complex with Inhbitor PG-895449'''
===Mutated MAP kinase P38 (Mus Musculus) in complex with Inhbitor PG-895449===




==Overview==
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A new class of tumor necrosis factor alpha (TNF-alpha) synthesis inhibitors based on an N-2,4-pyrimidine-N-phenyl-N'-phenyl urea scaffold is described. Many of these compounds showed low-nanomolar activity against lipopolysaccharide stimulated TNF-alpha production. X-ray co-crystallization studies with mutated p38alpha showed that these trisubstituted ureas interact with the ATP-binding pocket in a pseudo-bicyclic conformation brought about by the presence of an intramolecular hydrogen bonding interaction.
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{{ABSTRACT_PUBMED_16632356}}


==About this Structure==
==About this Structure==
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[[Category: Walter, R L.]]
[[Category: Walter, R L.]]
[[Category: Map kinase p38]]
[[Category: Map kinase p38]]
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Revision as of 14:25, 27 July 2008

File:2ghm.png

Template:STRUCTURE 2ghm

Mutated MAP kinase P38 (Mus Musculus) in complex with Inhbitor PG-895449Mutated MAP kinase P38 (Mus Musculus) in complex with Inhbitor PG-895449

Template:ABSTRACT PUBMED 16632356

About this StructureAbout this Structure

2GHM is a Single protein structure of sequence from Mus musculus. Full crystallographic information is available from OCA.

ReferenceReference

Development of N-2,4-pyrimidine-N-phenyl-N'-phenyl ureas as inhibitors of tumor necrosis factor alpha (TNF-alpha) synthesis. Part 1., Brugel TA, Maier JA, Clark MP, Sabat M, Golebiowski A, Bookland RG, Laufersweiler MJ, Laughlin SK, Vanrens JC, De B, Hsieh LC, Mekel MJ, Janusz MJ, Bioorg Med Chem Lett. 2006 Jul 1;16(13):3510-3. Epub 2006 May 2. PMID:16632356

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