Biological evaluation of Tyr6 and Ser7 modified drosocin analogues

被引：9

作者：

de Visser, PC

van Hooft, PAV

de Vries, AM

de Jong, A

van der Marel, GA

Overkleeft, HS

Noort, D

机构：

[1] TNO, Def, Secur & Safety, NL-2280 AA Rijswijk, Netherlands

[2] Leiden Univ, Leiden Inst Chem, NL-2300 RA Leiden, Netherlands

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 11期

关键词：

D O I：

10.1016/j.bmcl.2005.03.074

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An array of analogues of the cationic antimicrobial peptide drosocin was synthesized containing substitutions of Tyr6 and Ser7 in order to increase the proteolytic stability. Stabilizing the N-terminus with unnatural amino acids increased the serum stability of analogues by almost a factor 30 over an 8 h period. (c) 2005 Elsevier Ltd. All rights reserved.

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收藏

页码：2902 / 2905

页数：4

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