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糖苷酶研究中抑制剂的应用。

The use of inhibitors in the study of glycosidases.

作者信息

Lalégerie P, Legler G, Yon J M

出版信息

Biochimie. 1982 Nov-Dec;64(11-12):977-1000. doi: 10.1016/s0300-9084(82)80379-9.

Abstract

The use of non-covalent as well as covalent inhibitors can be a useful tool to approach the mechanism of activity of glycosidases. An efficient method to determine the essential amino-acid groups directly or indirectly involved in the catalytic process is the use of active site directed irreversible inhibitors. Epoxide derivatives from conduritol B and conduritol C are the most important inhibitors in this group. The use of active site reversible inhibitors: cationic and basic glycosyl derivatives, glycals, glyconolactones, thioglycosides, is effective to study the different charges at the active site or the transition state during catalysis and also to detect conformational adaptability of an enzyme. Furthermore, inhibitors can be valuable tools to investigate various aspects of the physiological role of glycosidases.

摘要

使用非共价和共价抑制剂可能是研究糖苷酶活性机制的有用工具。一种直接或间接确定参与催化过程的必需氨基酸基团的有效方法是使用活性位点导向的不可逆抑制剂。来自conduritol B和conduritol C的环氧化物衍生物是该组中最重要的抑制剂。使用活性位点可逆抑制剂:阳离子和碱性糖基衍生物、缩水甘油醛、糖醛酸内酯、硫代糖苷,对于研究催化过程中活性位点或过渡态的不同电荷以及检测酶的构象适应性是有效的。此外,抑制剂可能是研究糖苷酶生理作用各个方面的有价值工具。

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