Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A

被引：191

作者：

Walsh, AH ^{[1
]}

Cheng, AY ^{[1
]}

Honkanen, RE ^{[1
]}

机构：

[1] UNIV S ALABAMA, COLL MED, DEPT BIOCHEM & MOL BIOL, MOBILE, AL 36688 USA

来源：

FEBS LETTERS | 1997年 / 416卷 / 03期

关键词：

fostriecin; okadaic acid; cantharidin; serine/threonine; protein; phosphatase; inhibitor; dephosphorylation; toxin; tumor promotion; antitumor activity;

D O I：

10.1016/S0014-5793(97)01210-6

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 mu M) 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. (C) 1997 Federation of European Biochemical Societies.

引用

页码：230 / 234

页数：5

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