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Fostriecin, an Antitumor Antibiotic with Inhibitory Activity Against Serine/threonine Protein Phosphatases Types 1 (PP1) and 2A (PP2A), is Highly Selective for PP2A

Overview
Journal FEBS Lett
Specialty Biochemistry
Date 1997 Dec 31
PMID 9373158
Citations 65
Authors
A H Walsh
A Cheng
R E Honkanen
Affiliations
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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.

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