BENARTHIN - A NEW INHIBITOR OF PYROGLUTAMYL PEPTIDASE .3. SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS

被引：4

作者：

HATSU, M ^{[1
]}

TUDA, M ^{[1
]}

MURAOKA, Y ^{[1
]}

AOYAGI, T ^{[1
]}

TAKEUCHI, T ^{[1
]}

机构：

[1] SHOWA COLL PHARMACEUT SCI,DEPT HYG CHEM,MACHIDA,TOKYO 194,JAPAN

来源：

JOURNAL OF ANTIBIOTICS | 1992年 / 45卷 / 07期

关键词：

D O I：

10.7164/antibiotics.45.1088

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Benarthin, a new inhibitor of pyroglutamyl peptidase (PG-peptidase), has been isolated from the culture filtrate of Streptomyces xanthophaeus MJ244-SF1. The structure of benarthin has been determined to be L-(2,3-dihydroxybenzoyl)arginyl-L-threonine. This structure was confirmed by the total synthesis of benarthin. Moreover, we synthesized benarthin derivatives to obtain information on the relationship between structure and inhibitory activity. The results indicated that the catechol group of benarthin is the essential moiety for the inhibition of PG-peptidase.

引用

页码：1088 / 1095

页数：8

共 9 条

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