3fzf | pdb_00003fzf

Crystal Structure of Hsc70/Bag1 in complex with ATP

spinqualitylabelsall models 3fzf, resolution 2.20Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3fzf is a 2 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: ATP Related: 3fzh, 3fzk, 3fzl, 3fzm Gene: HSPA8, HSC70, HSP73, HSPA10 (Homo sapiens), BAG1, HAP (Homo sapiens) 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 The design and synthesis of novel adenosine-derived inhibitors of HSP70, guided by modeling and X-ray crystallographic structures of these compounds in complex with HSC70/BAG-1, is described. Examples exhibited submicromolar affinity for HSP70, were highly selective over HSP90, and some displayed potency against HCT116 cells. Exposure of compound 12 to HCT116 cells caused significant reduction in cellular levels of Raf-1 and Her2 at concentrations similar to that which caused cell growth arrest. Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design.,Williamson DS, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Foloppe N, Francis GL, Graham CJ, Howes R, Macias AT, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ J Med Chem. 2009 Mar 26;52(6):1510-3. PMID:19256508 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also BAG protein Heat Shock Proteins

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