喷他脒激活葡萄糖-6-磷酸酶系统的肝脏微粒体葡萄糖6-磷酸转运蛋白T1。

Pentamidine activates T1 the hepatic microsomal glucose 6-phosphate transport protein of the glucose-6-phosphatase system.

作者信息

Scott H M, Burchell A

机构信息

Department of Obstetrics and Gynaecology, Centre for Research into Human Development, Ninewells Hospital and Medical School, University of Dundee, U.K.

出版信息

Biochim Biophys Acta. 1991 Jul 26;1097(1):31-6. doi: 10.1016/0925-4439(91)90020-a.

DOI:10.1016/0925-4439(91)90020-a

PMID:1650253

Abstract

The mechanism of activation of hepatic microsomal glucose-6-phosphatase (EC 3.1.3.9) in vitro by pentamidine has been investigated in both intact and fully disrupted microsomes. The major effect of pentamidine is a 4.7-fold reduction in the Km of glucose-6-phosphatase activity in intact diabetic rat liver microsomes. The site of action of pentamidine is T1 the hepatic microsomal glucose 6-phosphate transport protein. The activation of T1 by pentamidine may contribute to the disturbed blood glucose homeostasis seen in many patients after the administration of the drug pentamidine.

摘要

已在完整和完全破碎的微粒体中研究了喷他脒在体外激活肝微粒体葡萄糖-6-磷酸酶（EC 3.1.3.9）的机制。喷他脒的主要作用是使完整糖尿病大鼠肝微粒体中葡萄糖-6-磷酸酶活性的Km降低4.7倍。喷他脒的作用位点是T1，即肝微粒体葡萄糖6-磷酸转运蛋白。喷他脒对T1的激活可能导致许多患者在使用喷他脒药物后出现血糖稳态紊乱。