Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition.

Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition. Research Abstract Details 

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Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition. Abstract Text:

Suzanne B Buck,Christophe Hardouin,Satoshi Ichikawa,Danielle R Soenen,C-M Gauss,Inkyu Hwang,Mark R Swingle,Kathy M Bonness,Richard E Honkanen,Dale L Boger,

Key derivatives and analogues of fostriecin were prepared and examined that revealed a fundamental role for the unsaturated lactone and confirmed the essential nature of the phosphate monoester. Thus, an identical 200-fold reduction in protein phosphatase 2A (PP2A) inhibition is observed with either the saturated lactone (7) or with an analogue that lacks the entire lactone (15). This 200-fold increase in PP2A inhibition attributable to the unsaturated lactone potentially may be due to reversible C269 alkylation within the PP beta12-beta13 active site loop accounting for PP2A/4 potency and selectivity.

Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition. Publishing Authors By Initials

SB Buck,C Hardouin,S Ichikawa,DR Soenen,CM Gauss,I Hwang,MR Swingle,KM Bonness,RE Honkanen,DL Boger,

For similar biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research abstracts see: biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research

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Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition. Journal Published:

PUBLICATION TYPE: Research Support, U.S. Gov't,

Journal: Journal of the American Chemical Society

VOLUME: 125

Page Numbers: 15694-5

Journal Abbreviation: J. Am. Chem. Soc.

ISSN: 0002-7863

DAY: 24

MONTH: Dec

YEAR: 2003

Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 7503056

Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition. Keywords Mesh Terms:

KEYWORDS: Structure-Activity Relationship

MESH TERMS: antagonists & inhibitors

Chemical & Substance for Abstract: Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition. Information

Substance Name: Phosphoprotein Phosphatases

Registry Number: EC 3.1.3.16

Grant and Affiliation Information for Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition.

AFFILIATION: Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.

Country: United States

AGENCY: United States NHLBI

GRANT: HL59154

ACRONYM: HL

MEDLINETA: J Am Chem Soc

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