4fa6 | pdb_00004fa6

Design and Synthesis of a Novel Pyrrolidinyl Pyrido Pyrimidinone Derivative as a Potent Inhibitor of PI3Ka and mTOR

spinqualitylabelsall models 4fa6, resolution 2.70Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4fa6 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: 0TA Related: 4fad Gene: PIK3CG (Homo sapiens) Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed Lead optimization efforts that employed structure base drug design and physicochemical property based optimization leading to the discovery of a novel series of 4-methylpyrido pyrimidinone (MPP) are discussed. Synthesis and profile of 1, a PI3Kalpha/mTOR dual inhibitor, is highlighted. Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kalpha and mTOR.,Le PT, Cheng H, Ninkovic S, Plewe M, Huang X, Wang H, Bagrodia S, Sun S, Knighton DR, LaFleur Rogers CM, Pannifer A, Greasley S, Dalvie D, Zhang E Bioorg Med Chem Lett. 2012 Aug 1;22(15):5098-103. doi:, 10.1016/j.bmcl.2012.05.100. Epub 2012 Jun 6. PMID:22749419 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Phosphoinositide 3-Kinases

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