Potential scorpionate antibiotics: targeted hydrolysis of lipid II containing model membranes by vancomycin–TACzyme conjugates and modulation of their antibacterial activity by Zn-ions
- Bauke Albada, H.
- Arnusch, C.J.
- Branderhorst, H.M.
- Verel, A-M.
- Janssen, W.T.M.
- Breukink, E.
- de Kruijff, B.
- Pieters, R.J.
- Liskamp, R.M.J.
DOIAbstract
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
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