myo-inositol 1,4,5-trisphosphorothioate is a potent competitive inhibitor of human erythrocyte 5-phosphatase

A M Cooke; S R Nahorski; B V Potter

doi:10.1016/0014-5793(89)80504-6

myo-inositol 1,4,5-trisphosphorothioate is a potent competitive inhibitor of human erythrocyte 5-phosphatase

FEBS Lett. 1989 Jan 2;242(2):373-7. doi: 10.1016/0014-5793(89)80504-6.

Authors

A M Cooke¹, S R Nahorski, B V Potter

Affiliation

¹ Department of Chemistry, University of Leicester, England.

PMID: 2536622
DOI: 10.1016/0014-5793(89)80504-6

Abstract

The effect of the myo-inositol 1,4,5-trisphosphate (IP3) analogue, myo-inositol 1,4,5-trisphosphorothioate (IPS3) on the dephosphorylation of D-5-[32P]IP3 by the 5-phosphatase from human erythrocyte membranes has been investigated. DL-IPS3 was found to act as a competitive inhibitor with a Ki of 6 microM, making it the most potent inhibitor currently available for this enzyme. L-IP3 inhibited the enzyme with a Ki of 124 microM and was more potent than D-2,3-diphosphoglycerate (Ki 978 microM).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Erythrocytes / enzymology
Humans
In Vitro Techniques
Inositol / analogs & derivatives*
Inositol / metabolism
Inositol / pharmacology
Inositol 1,4,5-Trisphosphate / analogs & derivatives
Inositol Polyphosphate 5-Phosphatases
Kinetics
Organothiophosphorus Compounds / metabolism*
Organothiophosphorus Compounds / pharmacology
Phosphoric Monoester Hydrolases / antagonists & inhibitors*

Substances

Organothiophosphorus Compounds
inositol 1,4,5-triphosphorothioate
Inositol
Inositol 1,4,5-Trisphosphate
Phosphoric Monoester Hydrolases
Inositol Polyphosphate 5-Phosphatases