Literature DB >> 3947331

Phenyl-n-butylborinic acid is a potent transition state analog inhibitor of lipolytic enzymes.

L D Sutton, J S Stout, L Hosie, P S Spencer, D M Quinn.   

Abstract

The cholesterol esterase and lipoprotein lipase catalyzed hydrolyses of the water-soluble substrate p-nitrophenyl butyrate are competitively inhibited by butaneboronic acid and phenylboronic acid. Phenyl-n-butylborinic acid has been synthesized and characterized as an ultrapotent transition state analog inhibitor: Ki = 2.9 +/- 0.6 nM and 1.7 +/- 0.3 microM for the cholesterol esterase and lipoprotein lipase reactions, respectively. These results are interpreted in terms of transition state structure and stabilization.

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Year:  1986        PMID: 3947331     DOI: 10.1016/0006-291x(86)90575-9

Source DB:  PubMed          Journal:  Biochem Biophys Res Commun        ISSN: 0006-291X            Impact factor:   3.575


  3 in total

1.  Acyl-CoA: cholesterol acyltransferase activity in the rat mammary gland: variation during pregnancy and lactation.

Authors:  J H Shand; D W West
Journal:  Lipids       Date:  1991-02       Impact factor: 1.880

2.  Proteus mirabilis urease. Partial purification and inhibition by boric acid and boronic acids.

Authors:  J M Breitenbach; R P Hausinger
Journal:  Biochem J       Date:  1988-03-15       Impact factor: 3.857

3.  An introduction to boron: history, sources, uses, and chemistry.

Authors:  W G Woods
Journal:  Environ Health Perspect       Date:  1994-11       Impact factor: 9.031

  3 in total

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