2zir | pdb_00002zir

Crystal Structure of rat protein farnesyltransferase complexed with a benzofuran inhibitor and FPP

spinqualitylabelsall models 2zir, resolution 2.40Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2zir is a 2 chain structure with sequence from Rattus norvegicus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: FPP, GOL, NH7, ZN Related: 2zis Gene: Fnta (Rattus norvegicus), Fntb (Rattus norvegicus) Activity: Protein farnesyltransferase, with EC number 2.5.1.58 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 A series of benzofuran-based farnesyltransferase inhibitors have been designed and synthesized as antitumor agents. Among them, 11f showed the most potent enzyme inhibitory activity (IC(50)=1.1nM) and antitumor activity in human cancer xenografts in mice. Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors.,Asoh K, Kohchi M, Hyoudoh I, Ohtsuka T, Masubuchi M, Kawasaki K, Ebiike H, Shiratori Y, Fukami TA, Kondoh O, Tsukaguchi T, Ishii N, Aoki Y, Shimma N, Sakaitani M Bioorg Med Chem Lett. 2009 Mar 15;19(6):1753-7. Epub 2009 Feb 11. PMID:19217288 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Farnesyltransferase

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