2gtm
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(New page: 200px<br /><applet load="2gtm" size="450" color="white" frame="true" align="right" spinBox="true" caption="2gtm, resolution 1.90Å" /> '''Mutated Mouse P38 MA...)
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Revision as of 09:15, 21 November 2007
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Mutated Mouse P38 MAP Kinase Domain in complex with Inhibitor PG-892579
Overview
A series of C-2, C-8, and N-9 trisubstituted purine based inhibitors of, TNF-alpha production are described. The most potent analogs showed low, nanomolar activity against LPS-induced TNF-alpha production in a THP-1, cell based assay. The SAR of the series was optimized with the aid of, X-ray co-crystal structures of these inhibitors bound with mutated p38, (mp38).
About this Structure
2GTM is a Single protein structure of sequence from Mus musculus with LID as ligand. Active as Mitogen-activated protein kinase, with EC number 2.7.11.24 Full crystallographic information is available from OCA.
Reference
The development of novel C-2, C-8, and N-9 trisubstituted purines as inhibitors of TNF-alpha production., Sabat M, Vanrens JC, Clark MP, Brugel TA, Maier J, Bookland RG, Laufersweiler MJ, Laughlin SK, Golebiowski A, De B, Hsieh LC, Walter RL, Mekel MJ, Janusz MJ, Bioorg Med Chem Lett. 2006 Aug 15;16(16):4360-5. Epub 2006 Jun 5. PMID:16750367
Page seeded by OCA on Wed Nov 21 11:23:04 2007
