2gtn | pdb_00002gtn

Mutated MAP kinase P38 (Mus Musculus) in complex with Inhbitor PG-951717

spinqualitylabelsall models 2gtn, resolution 1.80Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2gtn is a 1 chain structure with sequence from Mus musculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: LIE, SO4 Related: 1yw2, 1ywr, 2ghm, 2ghl Gene: Mapk14 (Mus musculus) Activity: Mitogen-activated protein kinase, with EC number 2.7.11.24 Resources: FirstGlance, OCA, RCSB, PDBsum Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed 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). 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 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Mitogen-activated protein kinase

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