2ghl

Mutant Mus Musculus P38 Kinase Domain in Complex with Inhibitor PG-874743Mutant Mus Musculus P38 Kinase Domain in Complex with Inhibitor PG-874743

Structural highlights 2ghl 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: Related: 1yw2, 1ywr Gene: Mapk14, Crk1, Csbp1, Csbp2 (Mus musculus) Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 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 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. 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 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Mitogen-activated protein kinase

spinqualitylabelsall models 2ghl, resolution 2.10Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image