Abstract
The role of the phosphatidylinositol 3-kinase (PI3K) pathway in the hyperphosphorylation of tau was investigated in SY5Y human neuroblastoma cells. Wortmannin, an inhibitor of PI3K, induced transient (after 1 h) activation of glycogen synthase kinase-3 (GSK-3), hyperphosphorylation of tau and dose-dependent cytotoxicity. However, continuous inactivation of protein kinase (PK) B was observed from 1 to 24 h, suggesting the involvement of protein kinase(s) other than PKB in the phosphorylation and inactivation of GSK-3 after 3 h. In cells treated with wortmannin, PKC delta fragments were observed, and the PKC activity increased after 3 h, whereas treatment of cells with z-DEVD-fmk, an inhibitor of caspase 3, also inhibited fragmentation of PKC delta and induced continuous activation of GSK-3. It is suggested that fragmentation of PKC delta during the process of apoptosis results in the phosphorylation and inactivation of GSK-3 and consequently inhibition of the phosphorylation of tau.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Alzheimer Disease / metabolism
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Androstadienes / pharmacology
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Apoptosis
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Calcium-Calmodulin-Dependent Protein Kinases / antagonists & inhibitors
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Calcium-Calmodulin-Dependent Protein Kinases / metabolism*
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Caspase 3
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Caspase Inhibitors
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Enzyme Inhibitors / pharmacology
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Glycogen Synthase Kinase 3
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Glycogen Synthase Kinases
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Humans
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Isoenzymes / pharmacology*
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Oligopeptides / pharmacology
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Phosphoinositide-3 Kinase Inhibitors
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Phosphorylation
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Protein Kinase C / pharmacology*
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Protein Kinase C-delta
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Signal Transduction / drug effects
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Tumor Cells, Cultured
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Wortmannin
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tau Proteins / metabolism*
Substances
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Androstadienes
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Caspase Inhibitors
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Enzyme Inhibitors
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Isoenzymes
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Oligopeptides
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Phosphoinositide-3 Kinase Inhibitors
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benzoylcarbonyl-aspartyl-glutamyl-valyl-aspartyl-fluoromethyl ketone
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tau Proteins
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Glycogen Synthase Kinases
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PRKCD protein, human
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Protein Kinase C
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Protein Kinase C-delta
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Calcium-Calmodulin-Dependent Protein Kinases
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Glycogen Synthase Kinase 3
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CASP3 protein, human
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Caspase 3
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Wortmannin