Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A.
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.
Walsh
A H
AH
Department of Biochemistry and Molecular Biology, College of Medicine, University of South Alabama, Mobile 36688, USA.
Cheng
A
A
Honkanen
R E
RE
D000475:Alkenes / Q000494:pharmacology; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology*; D001921:Brain / Q000201:enzymology; D002417:Cattle; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D007527:Isoenzymes / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D007700:Kinetics; D018482:Muscle, Skeletal / Q000201:enzymology; D019319:Okadaic Acid / Q000494:pharmacology; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D010764:Phosphorylase Kinase / Q000378:metabolism; D011090:Polyenes; D011753:Pyrones; D011817:Rabbits; D011993:Recombinant Fusion Proteins / Q000037:antagonists & inhibitors / Q000096:biosynthesis
D000475:Alkenes; D000903:Antibiotics, Antineoplastic; D004791:Enzyme Inhibitors; D007527:Isoenzymes; D011090:Polyenes; D011753:Pyrones; D011993:Recombinant Fusion Proteins; D019319:Okadaic Acid; D010764:Phosphorylase Kinase; D010749:Phosphoprotein Phosphatases; C040313:fostriecin