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Fostriecin is an inhibitor of the serine/threonine protein phosphatases 2A (PP2A) and 4 (PP4) (IC50s = 3.2 and 3 nM, respectively).1,2 It less effectively inhibits topoisomerase II and PP1 (IC50s = 40 and 131 μM, respectively) and does not inhibit PP2B.1,3 Through its effects on protein phosphatases, fostriecin increases the level of histone H3 phosphorylation and may alter epigenetic regulation of cell proliferation.4 On a related note, fostriecin was first identified as an antitumor antibiotic.5
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1. Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A. FEBS Lett. 416(3), 230-234 (1997).
2. Purification of protein phosphatase 4 catalytic subunit: Inhibition by the antitumour drug fostriecin and other tumour suppressors and promoters. FEBS Lett. 431(3), 357-361 (1998).
3. Serine-
4. Chemical regulation of epigenetic modifications: Opportunities for new cancer therapy. Med. Res. Rev. 28(5), 645-687 (2008).
5. Novel antitumor agents CI-