4ful | pdb_00004ful

PI3 Kinase Gamma bound to a pyrmidine inhibitor

spinqualitylabelsall models 4ful, resolution 2.47Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4ful is a 1 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: 0VU Gene: PIK3CG (Homo sapiens) Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed hSMG-1 kinase plays a dual role in a highly conserved RNA surveillance pathway termed nonsense-mediated RNA decay (NMD) and in cellular genotoxic stress response. Since deregulation of cellular responses to stress contributes to tumor growth and resistance to chemotherapy, hSMG-1 is a potential target for cancer treatment. From our screening efforts, we have identified pyrimidine derivatives as hSMG-1 kinase inhibitors. We report structure-based optimization of this pan-kinase scaffold to improve its biochemical profile and overall kinome selectivity, including mTOR and CDK, to generate the first reported selective hSMG-1 tool compound. Identification of pyrimidine derivatives as hSMG-1 inhibitors.,Gopalsamy A, Bennett EM, Shi M, Zhang WG, Bard J, Yu K Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41. doi: 10.1016/j.bmcl.2012.08.107., Epub 2012 Sep 7. PMID:23021994 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Phosphoinositide 3-Kinases

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