2ow3 | pdb_00002ow3

Glycogen synthase kinase-3 beta in complex with bis-(indole)maleimide pyridinophane inhibitor

spinqualitylabelsall models 2ow3, resolution 2.80Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2ow3 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: BIM NonStd Res: PTR Gene: GSK3B (Homo sapiens) Activity: [Tau_protein_kinase [Tau protein] kinase], with EC number 2.7.11.26 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 Novel bis(indolyl)maleimide pyridinophanes 3, 9a, 9b, 10a, 10b, and 11 were prepared by cobalt-mediated [2+2+2] cycloaddition of an appropriate alpha,omega-diyne with an N,N-dialkylcyanamide. These macrocyclic heterophanes were found to be potent, selective inhibitors of glycogen synthase kinase-3beta. An X-ray structure of a co-crystal of GSK-3beta and 3 (IC(50)=3nM) depicts the hydrogen bonding and hydrophobic interactions in the ATP-binding pocket of this serine/threonine protein kinase. Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.,Zhang HC, Bonaga LV, Ye H, Derian CK, Damiano BP, Maryanoff BE Bioorg Med Chem Lett. 2007 May 15;17(10):2863-8. Epub 2007 Feb 25. PMID:17350261 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Glycogen synthase kinase 3

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