Abstract
Fostriecin, an antitumor antibiotic produced by Streptomyces pulveraceus, is a strong inhibitor of type 2A (PP2A; IC50 3.2 nM) and a weak inhibitor of type 1 (PP1; IC50 131 microM) serine/threonine protein phosphatases. Fostriecin has no apparent effect on the activity of PP2B, and dose-inhibition studies conducted with whole cell homogenates indicate that fostriecin also inhibits the native forms of PP1 and PP2A. Studies with recombinant PP1/PP2A chimeras indicate that okadaic acid and fostriecin have different binding sites.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Alkenes / pharmacology
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Animals
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Antibiotics, Antineoplastic / pharmacology*
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Brain / enzymology
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Cattle
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Enzyme Inhibitors / pharmacology*
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Isoenzymes / antagonists & inhibitors
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Isoenzymes / biosynthesis
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Kinetics
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Muscle, Skeletal / enzymology
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Okadaic Acid / pharmacology
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Phosphoprotein Phosphatases / antagonists & inhibitors*
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Phosphoprotein Phosphatases / biosynthesis
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Phosphorylase Kinase / metabolism
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Polyenes
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Pyrones
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Rabbits
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Recombinant Fusion Proteins / antagonists & inhibitors
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Recombinant Fusion Proteins / biosynthesis
Substances
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Alkenes
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Antibiotics, Antineoplastic
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Enzyme Inhibitors
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Isoenzymes
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Polyenes
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Pyrones
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Recombinant Fusion Proteins
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Okadaic Acid
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Phosphorylase Kinase
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Phosphoprotein Phosphatases
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fostriecin