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

  作者 Albada, HB; Arnusch, CJ; Branderhorst, HM; Verel, AM; Janssen, WTM; Breukink, E; de Kruijff, B; Pieters, RJ; Liskamp, RMJ  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-14;  页码  3721-3724  
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[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.

 
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