Synthesis and characterization of the colistin peptide polymyxin E1 and related antimicrobial peptides

被引：7

作者：

Kline, T ^{[1
]}

Holub, D ^{[1
]}

Therrien, J ^{[1
]}

Leung, T ^{[1
]}

Ryckman, D ^{[1
]}

机构：

[1] PathoGenesis Corp, Seattle, WA 98119 USA

来源：

JOURNAL OF PEPTIDE RESEARCH | 2001年 / 57卷 / 03期

关键词：

cationic antimicrobial peptide; colistin; lariat peptide; polymyxin; solid-phase peptide synthesis;

D O I：

10.1046/j.1397-002X.2,000.00000.x

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Two strategies were developed to synthesize the acylated cyclic peptides know as polymyxins. Synthesis of polymyxin El and several analogs enabled us to evaluate the minimum inhibitory concentration of individual compounds against Gram-negative bacteria. In this study we also report the first identification of two component peptides in the complex polymyxin fermentation product colistin, a Thr2Ser isoform and an acyl group isomer. Both of these peptides, as well as a known component peptide, Leu7lle, were similar to polymyxin E1 in potency, suggesting that conservative mutations in the colistin family are functionally inconsequential. In contrast, the acyclic analogs of all of these peptides were inactive, indicating that the characteristic lariat structure of the polymyxins is necessary for antimicrobial activity.

引用

页码：175 / 187

页数：13

共 38 条

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