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肌醇1,4,5-三硫代磷酸酯是一种有效的人红细胞5-磷酸酶竞争性抑制剂。

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

作者信息

Cooke A M, Nahorski S R, Potter B V

机构信息

Department of Chemistry, University of Leicester, England.

出版信息

FEBS Lett. 1989 Jan 2;242(2):373-7. 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).

摘要

已对肌醇1,4,5 - 三磷酸(IP3)类似物肌醇1,4,5 - 三硫代磷酸酯(IPS3)对人红细胞膜5 - 磷酸酶催化D - 5 - [32P]IP3去磷酸化作用进行了研究。发现DL - IPS3作为竞争性抑制剂,其抑制常数Ki为6微摩尔,是目前该酶最有效的抑制剂。L - IP3抑制该酶的Ki为124微摩尔,比D - 2,3 - 二磷酸甘油酸(Ki 978微摩尔)更有效。

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