The vancomycin-nisin(1-12) hybrid restores activity against vancomycin resistant enterococci

Christopher J. Arnusch; Alexandre M.J.J. Bonvin; Anne Marie Verel; Wouter T.M. Jansen; Rob M.J. Liskamp; Ben De Kruijff; Roland J. Pieters; Eefjan Breukink

doi:10.1021/bi801597b

The vancomycin-nisin(1-12) hybrid restores activity against vancomycin resistant enterococci

Christopher J. Arnusch, Alexandre M.J.J. Bonvin, Anne Marie Verel, Wouter T.M. Jansen, Rob M.J. Liskamp, Ben De Kruijff, Roland J. Pieters, Eefjan Breukink

Research output: Contribution to journal › Article › peer-review

74 Scopus citations

Abstract

Lipid II is a crucial component in bacterial cell wall synthesis [Breukink, E., et al. (1999) Science 286, 2361-2364]. It is the target of a number of important antibiotics, which include vancomycin and nisin [Breukink, E., and de Kruijff, B. (2006) Nat. Rev. Drug Discovery 5, 321-332]. Here we show that a hybrid antibiotic that consists of vancomycin and nisin fragments is significantly more active than the separate fragments against vancomycin resistant entercocci (VRE). Three different hybrids were synthesized using click chemistry and compared. Optimal spacer lengths and connection points were predicted using computer modeling.

Original language	English
Pages (from-to)	12661-12663
Number of pages	3
Journal	Biochemistry
Volume	47
Issue number	48
DOIs	https://doi.org/10.1021/bi801597b
State	Published - 2 Dec 2008
Externally published	Yes

ASJC Scopus subject areas

Biochemistry

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10.1021/bi801597b

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title = "The vancomycin-nisin(1-12) hybrid restores activity against vancomycin resistant enterococci",

abstract = "Lipid II is a crucial component in bacterial cell wall synthesis [Breukink, E., et al. (1999) Science 286, 2361-2364]. It is the target of a number of important antibiotics, which include vancomycin and nisin [Breukink, E., and de Kruijff, B. (2006) Nat. Rev. Drug Discovery 5, 321-332]. Here we show that a hybrid antibiotic that consists of vancomycin and nisin fragments is significantly more active than the separate fragments against vancomycin resistant entercocci (VRE). Three different hybrids were synthesized using click chemistry and compared. Optimal spacer lengths and connection points were predicted using computer modeling.",

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AU - Arnusch, Christopher J.

AU - Bonvin, Alexandre M.J.J.

AU - Verel, Anne Marie

AU - Jansen, Wouter T.M.

AU - Liskamp, Rob M.J.

AU - De Kruijff, Ben

AU - Pieters, Roland J.

AU - Breukink, Eefjan

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The vancomycin-nisin(1-12) hybrid restores activity against vancomycin resistant enterococci

Abstract

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