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

C.J. Arnusch; A.M.J.J. Bonvin; A.M. Verel; W.T.M. Jansen; R.M.J. Liskamp; B. de Kruijff; R.J. Pieters; E.J. Breukink

doi:10.1021/bi801597b

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

C.J. Arnusch, A.M.J.J. Bonvin, A.M. Verel, W.T.M. Jansen, R.M.J. Liskamp, B. de Kruijff, R.J. Pieters, E.J. Breukink

University Medical Center Utrecht

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

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	Undefined/Unknown
Pages (from-to)	12661-12663
Number of pages	3
Journal	Biochemistry
Volume	47
Issue number	48
DOIs	https://doi.org/10.1021/bi801597b
Publication status	Published - 2008

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Cite this

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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.",

author = "C.J. Arnusch and A.M.J.J. Bonvin and A.M. Verel and W.T.M. Jansen and R.M.J. Liskamp and {de Kruijff}, B. and R.J. Pieters and E.J. Breukink",

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AU - Arnusch, C.J.

AU - Bonvin, A.M.J.J.

AU - Verel, A.M.

AU - Jansen, W.T.M.

AU - Liskamp, R.M.J.

AU - de Kruijff, B.

AU - Pieters, R.J.

AU - Breukink, E.J.

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AB - 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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