Potential scorpionate antibiotics: Targeted hydrolysis of lipid II containing model membranes by vancomycin-TACzyme conjugates and modulation of their antibacterial activity by Zn-ions

被引：4

作者：

Albada, H. Bauke ^{[1
]}

Arnusch, Christopher J. ^{[1
,2
]}

Branderhorst, Hilbert M. ^{[1
]}

Verel, Anne-Marie ^{[3
]}

Janssen, Wouter T. M. ^{[3
]}

Breukink, Eefjan ^{[2
]}

de Kruijff, Ben ^{[2
]}

Pieters, Roland J. ^{[1
]}

Liskamp, Rob M. J. ^{[1
]}

机构：

[1] Univ Utrecht, Utrecht Inst Pharmaceut Sci, Dept Med Chem & Chem Biol, NL-3508 TB Utrecht, Netherlands

[2] Univ Utrecht, Dept Chem Biol & Organ Chem, Biomembrane Inst, Bijvoet Ctr Biomol Res,Sci Fac, NL-3584 CH Utrecht, Netherlands

[3] Univ Med Ctr Utrecht, Dept Med Microbiol, NL-3584 CX Utrecht, Netherlands

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 14期

关键词：

Hydrolytic enzyme mimic; Vancomycin; Antibiotic; Click chemistry; Dendrimer; CELL-WALL; MOLECULES; AZIDES;

D O I：

10.1016/j.bmcl.2009.05.064

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The antibiotic vancomycin-that binds lipid II in the bacterial cell membrane-was conjugated to a mono- and tetravalent mimic of the tris-histidine catalytic triad of metalloenzymes. Targeted hydrolysis by the conjugate was observed using model membranes containing lipid II, and in vitro MIC-values of the targeted mimic constructs could be modulated by Zn-ions. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：3721 / 3724

页数：4

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