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

共 46 条

[1] ACTIVATION OF PROTEIN-KINASES AND INHIBITION OF PROTEIN PHOSPHATASES PLAY A CENTRAL ROLE IN THE REGULATION OF EXOCYTOSIS IN MOUSE PANCREATIC BETA-CELLS [J].

AMMALA, C ;

ELIASSON, L ;

BOKVIST, K ;

BERGGREN, PO ;

HONKANEN, RE ;

SJOHOLM, A ;

RORSMAN, P .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1994, 91 (10) :4343-4347

[2] A molecular basis for different interactions of marine toxins with protein phosphatase-1 - Molecular models for bound motuporin, microcystins, okadaic acid, and calyculin A [J].

Bagu, JR ;

Sykes, BD ;

Craig, MM ;

Holmes, CFB .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1997, 272 (08) :5087-5097

[3]

BARIK S, 1995, METH NEUROSCI, V26, P309

[4] INHIBITORY EFFECT OF A MARINE-SPONGE TOXIN, OKADAIC ACID, ON PROTEIN PHOSPHATASES - SPECIFICITY AND KINETICS [J].

BIALOJAN, C ;

TAKAI, A .

BIOCHEMICAL JOURNAL, 1988, 256 (01) :283-290

[5] INHIBITION OF TYPE-II TOPOISOMERASE BY FOSTRIECIN [J].

BORITZKI, TJ ;

WOLFARD, TS ;

BESSERER, JA ;

JACKSON, RC ;

FRY, DW .

BIOCHEMICAL PHARMACOLOGY, 1988, 37 (21) :4063-4068

[6]

BRAUTIGAN DL, 1988, METHOD ENZYMOL, V159, P339

[7]

BRAUTIGAN DL, 1985, J BIOL CHEM, V260, P4295

[8] NAMING OF CYCLIC HEPTAPEPTIDE TOXINS OF CYANOBACTERIA (BLUE-GREEN-ALGAE) [J].

CARMICHAEL, WW ;

BEASLEY, V ;

BUNNER, DL ;

ELOFF, JN ;

FALCONER, I ;

GORHAM, P ;

HARADA, KI ;

KRISHNAMURTHY, T ;

YU, MJ ;

MOORE, RE ;

RINEHART, K ;

RUNNEGAR, M ;

SKULBERG, OM ;

WATANABE, M .

TOXICON, 1988, 26 (11) :971-973

[9]

CHEN SC, 1990, J ANTIBIOT, V63, P809

[10] THE STRUCTURE AND REGULATION OF PROTEIN PHOSPHATASES [J].

COHEN, P .

ANNUAL REVIEW OF BIOCHEMISTRY, 1989, 58 :453-508

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