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PDBsum entry 3f88
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References listed in PDB file
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Key reference
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Title
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Design, Synthesis and structure-Activity relationships of 1,3,4-Oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.
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Authors
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M.Saitoh,
J.Kunitomo,
E.Kimura,
Y.Hayase,
H.Kobayashi,
N.Uchiyama,
T.Kawamoto,
T.Tanaka,
C.D.Mol,
D.R.Dougan,
G.S.Textor,
G.P.Snell,
F.Itoh.
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Ref.
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Bioorg Med Chem Lett, 2009,
17,
2017-2029.
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PubMed id
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Abstract
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Glycogen 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.
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