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天冬氨酸和谷氨酸的膦酸及次膦酸类似物对氨肽酶的抑制作用

Inhibition of aminopeptidases by phosphonic acid and phosphinic acid analogues of aspartic and glutamic acids.

作者信息

Lejczak B, De Choszczak M P, Kafarski P

机构信息

Institute of Organic and Physical Chemistry, Technical University of Wroclaw, Poland.

出版信息

J Enzyme Inhib. 1993;7(2):97-103. doi: 10.3109/14756369309040752.

Abstract

More than 30 phosphonic and phosphinic acid analogues of aspartic and glutamic acids were synthesized in order to probe how the structural differences of these molecules were reflected in their ability to inhibit cytosolic (LAP) and microsomal (APM) aminopeptidases. Although most of the compounds studied were found to exert only a modest inhibitory effect, the studies provide some information on the structural requirements of the binding subsites and catalytic centers of both enzymes.

摘要

为了探究天冬氨酸和谷氨酸的30多种膦酸和次膦酸类似物的结构差异如何体现在它们抑制胞质(LAP)和微粒体(APM)氨肽酶的能力上,合成了这些类似物。尽管所研究的大多数化合物仅表现出适度的抑制作用,但这些研究为两种酶的结合亚位点和催化中心的结构要求提供了一些信息。

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