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哌拉他汀B:一种来自薰衣草链霉菌MJ908-WF13的新型选择性丝氨酸羧肽酶抑制剂。

Piperastatin B: a new selective serine carboxypeptidase inhibitor from Streptomyces lavendofoliae MJ908-WF13.

作者信息

Murakami S, Harada S, Takahashi Y, Naganawa H, Takeuchi T, Aoyagi T

机构信息

Institute of Microbial Chemistry, Tokyo, Japan.

出版信息

J Enzyme Inhib. 1996 Aug;11(1):51-66. doi: 10.3109/14756369609038222.

Abstract

Piperastatin B, a new inhibitor of serine carboxypeptidase was purified from a culture broth of Streptomyces lavendofoliae MJ908-WF13 as a minor component by monitoring its inhibitory activity against carboxypeptidase Y (CP-Y). Its structure was determined to be N-formyl-Val-Thr-Leu-Val-Pip-Leu-Pip (pip: piperazic acid, hexahydropyridadine-3-carboxylic acid). Piperastatin B is a highly specific competitive inhibitor of CP-Y (Ki = 55 nM) with little effect on related enzymes and resembles the major component, piperastatin A, in these respects.

摘要

哌拉他汀B是一种新型丝氨酸羧肽酶抑制剂,从薰衣草链霉菌MJ908-WF13的培养液中作为次要成分纯化得到,通过监测其对羧肽酶Y(CP-Y)的抑制活性来实现。其结构确定为N-甲酰基-Val-Thr-Leu-Val-Pip-Leu-Pip(pip:哌嗪酸,六氢吡啶-3-羧酸)。哌拉他汀B是CP-Y的高度特异性竞争性抑制剂(Ki = 55 nM),对相关酶影响很小,在这些方面与主要成分哌拉他汀A相似。

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