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

FEBS Letters

Walsh, Aimée H.¹  Cheng, Aiyang¹  Honkanen, Richard E.¹ 

[1] Department of Biochemistry and Molecular Biology, MSB2198, College of Medicine, University of South Alabama, Mobile, AL 36688, USA

关键词: Fostriecin;    Okadaic acid;    Cantharidin;    Serine/threonine;    Protein;    Phosphatase;    Inhibitor;    Dephosphorylation;    Toxin;    Tumor promotion;    Antitumor activity;   

DOI  :  10.1016/S0014-5793(97)01210-6

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 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 μM) 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.

【 授权许可】

Unknown