3f7z
From Proteopedia
X-ray Co-Crystal Structure of Glycogen Synthase Kinase 3beta in Complex with an Inhibitor
Structural highlights
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 PubMedGlycogen synthase kinase-3beta (GSK-3beta) is implicated in abnormal hyperphosphorylation of tau protein and its inhibitors are expected to be a promising therapeutic agents for the treatment of Alzheimer's disease. Here we report design, synthesis and structure-activity relationships of a novel series of oxadiazole derivatives as GSK-3beta inhibitors. Among these inhibitors, compound 20x showed highly selective and potent GSK-3beta inhibitory activity in vitro and its binding mode was determined by obtaining the X-ray co-crystal structure of 20x and GSK-3beta. Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.,Saitoh M, Kunitomo J, Kimura E, Hayase Y, Kobayashi H, Uchiyama N, Kawamoto T, Tanaka T, Mol CD, Dougan DR, Textor GS, Snell GP, Itoh F Bioorg Med Chem. 2009 Mar 1;17(5):2017-29. Epub 2009 Jan 15. PMID:19200745[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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