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锥虫中糖酵解酶的抑制作用:寄生虫病治疗新先导物开发的一种方法。

Inhibition of the glycolytic enzymes in the trypanosome: an approach in the development of new leads in the therapy of parasitic diseases.

作者信息

Perie J, Riviere-Alric I, Blonski C, Gefflaut T, Lauth de Viguerie N, Trinquier M, Willson M, Opperdoes F R, Callens M

机构信息

Groupe de Chimie Organique Biologique, URA au CNRS 470, Université Paul Sabatier, Toulouse, France.

出版信息

Pharmacol Ther. 1993 Nov;60(2):347-65. doi: 10.1016/0163-7258(93)90016-7.

Abstract

Glycolysis in the trypanosome represents an important target for the development of new therapeutic agents due to the fact that this metabolism is essential for the parasite, glucose being its sole source of energy. In addition, different features of this metabolism and those associated with glycolytic enzymes offer opportunities for the development of efficient and selective compounds. Examples are given in this work of inhibitors directed to the enzymes aldolase and glyceraldehyde-phosphate-dehydrogenase and also of molecules acting specifically on the clusters of basic amino-acids present at the surfaces of the glycolytic enzymes in the parasite.

摘要

由于糖酵解代谢对锥虫至关重要(葡萄糖是其唯一能量来源),锥虫中的糖酵解成为开发新型治疗药物的重要靶点。此外,这种代谢以及与糖酵解酶相关的不同特征为开发高效且具选择性的化合物提供了机会。本文给出了针对醛缩酶和甘油醛 - 磷酸脱氢酶的抑制剂的实例,以及专门作用于寄生虫糖酵解酶表面碱性氨基酸簇的分子的实例。

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