4kin | pdb_00004kin

Crystal structure of mitogen-activated protein kinase 14 (P38-H5) complex with 5-(2-CHLOROPHENYL)-N-(5-(CYCLOPROPYLCARBAMOYL)-2-METHYLPHENYL)-2-THIOPHENECARBOXAMIDE

spinqualitylabelsall models 4kin, resolution 1.97Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4kin is a 4 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 1M8 Related: 4kip, 4kiq Gene: CSBP, CSBP1, CSBP2, CSPB1, MAPK14, MXI2, SAPK2A (Homo sapiens) Activity: Mitogen-activated protein kinase, with EC number 2.7.11.24 Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed A novel series of p38 MAP kinase inhibitors with high selectivity for the p38alpha isoform over the other family members including the highly homologous p38beta isoform has been identified. X-ray co-crystallographic studies have revealed an unprecedented kinase binding mode in p38alpha for representative analogs, 5c and 9d, in which a Leu108/Met109 peptide flip occurs within the p38alpha hinge region. Based on these findings, a general strategy for the rational design of additional promising p38alpha isoform selective inhibitors by targeting this novel binding mode is proposed. The identification of novel p38alpha isoform selective kinase inhibitors having an unprecedented p38alpha binding mode.,Wrobleski ST, Lin S, Murali Dhar TG, Dyckman AJ, Li T, Pitt S, Zhang R, Fan Y, Doweyko AM, Tokarski JS, Kish KF, Kiefer SE, Sack JS, Newitt JA, Witmer MR, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K Bioorg Med Chem Lett. 2013 Jul 15;23(14):4120-6. doi: 10.1016/j.bmcl.2013.05.047., Epub 2013 May 23. PMID:23746475 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Mitogen-activated protein kinase

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