myo‐Inositol 1,4,5‐trisphosphorothioate is a potent competitive inhibitor of human erythrocyte 5‐phosphatase

FEBS Letters

Cooke, Allan M.¹  Potter, Barry V.L.¹  Nahorski, Stefan R.² 

[1] Departments of Chemistry, University of Leicester, Leicester LE1 7RH, England;Pharmacology, University of Leicester, Leicester LE1 7RH, England

关键词: Second messenger;    Inositol phosphate;    Inhibitor;    Phosphatase;   

DOI  :  10.1016/0014-5793(89)80504-6

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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 K _i of 6 μM, making it the most potent inhibitor currently available for this enzyme. L-IP₃ inhibited the enzyme with a K _i of 124 μM and was more potent than D-2,3-diphosphoglycerate (K _i 978 μM).

【 授权许可】

Unknown