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[一种合成酶抑制剂的新方法]

[A new approach to the synthesis of enzyme inhibitors].

作者信息

Kritsyn A M, Mikhaĭlov S N, Florent'ev V L

出版信息

Mol Biol (Mosk). 1975 Jan-Feb;9(1):121-5.

PMID:1219366
Abstract

On the basis of the application of transition-state theory to enzymatic catalysis a novel approach to the synthesis of inhibitors of enzymes involving conformational rigid substrate has been proposed. It is predicted that the substrates which resemble the natural species in the structure of functional groups, but posses conformational flexibility, will be bound to the enzyme more tightly and converted more slowly than the natural substrate.

摘要

基于过渡态理论在酶催化中的应用,提出了一种合成涉及构象刚性底物的酶抑制剂的新方法。据预测,在官能团结构上与天然底物相似,但具有构象灵活性的底物,与酶的结合将比天然底物更紧密,转化速度更慢。

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