3ksq | pdb_00003ksq

Discovery of C-Imidazole Azaheptapyridine FPT Inhibitors

spinqualitylabelsall models 3ksq, resolution 2.10Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3ksq is a 2 chain structure with sequence from Buffalo rat. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: FPP, MG, Z96, ZN Gene: Fnta (Buffalo rat), Fntb (Buffalo rat) Activity: Protein farnesyltransferase, with EC number 2.5.1.58 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function [FNTB_RAT] Catalyzes the transfer of a farnesyl moiety from farnesyl pyrophosphate to a cysteine at the fourth position from the C-terminus of several proteins. The beta subunit is responsible for peptide-binding. 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 discovery of C-linked imidazole azaheptapyridine bridgehead FPT inhibitors is described. This novel class of compounds are sub nM FPT enzyme inhibitors with potent cellular inhibitory activities. This series also has reduced hERG activity versus previous N-linked imidazole series. X-ray of compound 10a bound to FTase revealed strong interaction between bridgehead imidazole 3N with catalytic zinc atom. Discovery of C-imidazole azaheptapyridine FPT inhibitors.,Zhu HY, Cooper AB, Desai J, Njoroge G, Kirschmeier P, Bishop WR, Strickland C, Hruza A, Doll RJ, Girijavallabhan VM Bioorg Med Chem Lett. 2010 Feb 1;20(3):1134-6. Epub 2009 Dec 6. PMID:20056542 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Farnesyltransferase

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