ホストリエシン

効能

抗悪性腫瘍薬

説明

Fostriecin is an inhibitor of the serine/threonine protein phosphatases 2A (PP2A) and 4 (PP4) (IC₅₀s = 3.2 and 3 nM, respectively). It less effectively inhibits topoisomerase II and PP1 (IC₅₀s = 40 and 131 μM, respectively) and does not inhibit PP2B. Through its effects on protein phosphatases, fostriecin increases the level of histone H3 phosphorylation and may alter epigenetic regulation of cell proliferation. On a related note, fostriecin was first identified as an antitumor antibiotic.

使用

Antineoplastic. Fostriecin is a Topo II, PP1, and PP2A inhibitor.

生物活性

Originally identified as an antitumor antibiotic from Streptomyces pulveraceous . Displays potent inhibition of protein phosphatase types 2A (PP2A) and 4 (PP4) with IC 50 values of 1.5 nM and 3 nM respectively. Also exhibits weaker inhibition of topoisomerase II (IC 50 = 40 μ M) and protein phosphatase type 1 (PP1) (IC 50 = 131 μ M) with no apparent inhibition of protein phosphatase type 2B (PP2B). Active in vivo .