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

Arnusch, C.J., Bonvin, A.M.J.J., Verel, A.M., Jansen, W.T.M., Liskamp, R.M.J. , de Kruijff, B., Pieters, R.J. and Breukink, E. (2008) The vancomycin−nisin(1−12)hybrid restores activity against vancomycin resistant enterococci. Biochemistry, 47(48), pp. 12661-12663. (doi: 10.1021/bi801597b)

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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.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Liskamp, Professor Robert
Authors: Arnusch, C.J., Bonvin, A.M.J.J., Verel, A.M., Jansen, W.T.M., Liskamp, R.M.J., de Kruijff, B., Pieters, R.J., and Breukink, E.
College/School:College of Science and Engineering > School of Chemistry
Journal Name:Biochemistry
ISSN:0006-2960
ISSN (Online):1520-4995

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