3r7r | pdb_00003r7r

Structure-based design of thienobenzoxepin inhibitors of PI3-Kinase

spinqualitylabelsall models 3r7r, resolution 2.90Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3r7r 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: FAZ Related: 3r7q Gene: PIK3CG (Homo sapiens) Activity: Phosphatidylinositol-4,5-bisphosphate 3-kinase, with EC number 2.7.1.153 Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed Starting from thienobenzopyran HTS hit 1, co-crystallization, molecular modeling and metabolic analysis were used to design potent and metabolically stable inhibitors of PI3-kinase. Compound 15 demonstrated PI3K pathway suppression in a mouse MCF7 xenograft model. Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.,Staben ST, Siu M, Goldsmith R, Olivero AG, Do S, Burdick DJ, Heffron TP, Dotson J, Sutherlin DP, Zhu BY, Tsui V, Le H, Lee L, Lesnick J, Lewis C, Murray JM, Nonomiya J, Pang J, Prior WW, Salphati L, Rouge L, Sampath D, Sideris S, Wiesmann C, Wu P Bioorg Med Chem Lett. 2011 Jul 1;21(13):4054-8. Epub 2011 May 13. PMID:21636270 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Phosphoinositide 3-Kinases

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