氨基酸与肽。三十九。肌氨酸-谷氨酰胺-缬氨酸-缬氨酸-丙氨酸-丙氨酸-对硝基苯胺的合成及其对巯基蛋白酶的作用。

Amino acids and peptides. XXXIX. Synthesis of iNoc-Gln-Val-Val-Ala-Ala-pNA and its action on thiol proteinases.

作者信息

Okada Y, Tsuda Y, Mu Y, Hirano K, Okamoto H, Okamoto Y, Kakegawa H, Matsumoto H, Sato T

机构信息

Faculty of Pharmaceutical Sciences, Kobe-Gakuin University, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1995 Jan;43(1):96-9. doi: 10.1248/cpb.43.96.

DOI:10.1248/cpb.43.96

Abstract

Based on the results of X-ray analysis of the complex between Suc-Gln-Val-Val-Ala-Ala-pNA, a fairly potent thiol proteinase inhibitor, and papain, iNoc-Gln-Val-Val-Ala-Ala-pNA was designed and prepared and its inhibitory activity against thiol proteinases was examined. iNoc-Gln-Val-Val-Ala-Ala-pNA inhibited cathepsin L fairly specifically, although its potency is not high.

摘要

基于对一种相当有效的巯基蛋白酶抑制剂Suc-Gln-Val-Val-Ala-Ala-pNA与木瓜蛋白酶复合物的X射线分析结果，设计并制备了iNoc-Gln-Val-Val-Ala-Ala-pNA，并检测了其对巯基蛋白酶的抑制活性。iNoc-Gln-Val-Val-Ala-Ala-pNA对组织蛋白酶L有相当特异性的抑制作用，尽管其效力不高。

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