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

Bioorganic & Medicinal Chemistry Letters
H Bauke AlbadaRob M J Liskamp

Abstract

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.

References

Sep 1, 1976·Nucleic Acids Research·I L CartwrightV W Armstrong
Dec 22, 1999·Science·Eefjan BreukinkBen de Kruijff
Oct 14, 2005·Journal of Medicinal Chemistry·Richard Morphy, Zoran Rankovic
Mar 15, 2006·Nature Reviews. Drug Discovery·Eefjan Breukink, Ben de Kruijff
Jul 8, 2008·Chembiochem : a European Journal of Chemical Biology·Hilbert M BranderhorstRoland J Pieters
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Citations

Jan 17, 2012·Journal of Medicinal Chemistry·Christopher J ArnuschYechiel Shai

Related Concepts

Lipid II
Antibiotics
Catalysis
Plasma Membrane
Hydrolysis
Imidazoles
Fungus Drug Sensitivity Tests
Uridine Diphosphate N-Acetylmuramic Acid
AB-Vancomycin
Bicyclo Compounds, Heterocyclic

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