The vancomycin-nisin(1-12) hybrid restores activity against vancomycin resistant enterococci
| Autor: | 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., Breukink, E.J., Biochemie van Membranen, Chemical Biology & Organic Chemistry, Medicinal Chemistry, NMR-spectroscopie, SYNTHESE, Dep Farmaceutische wetenschappen, Dep Scheikunde |
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| Rok vydání: | 2008 |
| Předmět: |
Models
Molecular medicine.drug_class Antibiotics Molecular Conformation Microbial Sensitivity Tests Biology Biochemistry Bacterial cell structure Microbiology chemistry.chemical_compound Vancomycin Vancomycin resistant Taverne medicine Nisin Lipid II Vancomycin Resistance Vancomycin-Resistant Enterococci biochemical phenomena metabolism and nutrition Uridine Diphosphate N-Acetylmuramic Acid Anti-Bacterial Agents Drug Combinations chemistry Click chemistry Enterococcus medicine.drug |
| Zdroj: | Biochemistry, 47(48), 12661. American Chemical Society : Division of Carbohydrate Chemistry |
| ISSN: | 0006-2960 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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