2ghl
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(New page: 200px<br /><applet load="2ghl" size="450" color="white" frame="true" align="right" spinBox="true" caption="2ghl, resolution 2.099Å" /> '''Mutant Mus Musculus...)
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Revision as of 09:05, 21 November 2007
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Mutant Mus Musculus P38 Kinase Domain in Complex with Inhibitor PG-874743
Overview
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.
About this Structure
2GHL is a Single protein structure of sequence from Mus musculus with LIB as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.
Reference
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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