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

Biochemistry
Christopher J ArnuschEefjan Breukink

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.

Citations

Jun 8, 2010·Journal of Medicinal Chemistry·Jed F Fisher, Shahriar Mobashery
Jan 17, 2012·Journal of Medicinal Chemistry·Christopher J ArnuschYechiel Shai
Jul 7, 2012·PloS One·Christopher J ArnuschEefjan Breukink
Sep 1, 2009·Future Medicinal Chemistry·Daniel D Long, Daniel G Marquess
May 26, 2015·Expert Opinion on Drug Discovery·Jerome Escano, Leif Smith
Sep 1, 2010·Expert Opinion on Drug Discovery·Varvara Pokrovskaya, Timor Baasov
Feb 24, 2015·Expert Opinion on Drug Discovery·Stephanie Kate Sandiford
Jun 12, 2012·Expert Opinion on Drug Discovery·Manuel Montalbán-LópezO P Kuipers
Dec 5, 2015·Journal of Medicinal Chemistry·Stephen A CochraneJohn C Vederas
Oct 26, 2010·Trends in Biotechnology·Srdjan JoveticJohannes Tramper
Dec 8, 2015·Frontiers in Microbiology·Des FieldR Paul Ross
Sep 12, 2013·Journal of Peptide Science : an Official Publication of the European Peptide Society·Jack C SlootwegDirk T S Rijkers
Nov 3, 2015·Biochimica Et Biophysica Acta·Sabine F OppedijkEefjan Breukink
Jun 13, 2015·Organic & Biomolecular Chemistry·Nigam M MishraErik V Van der Eycken
Apr 25, 2012·Biochimica Et Biophysica Acta·Cristina ChamorroRoland J Pieters
Dec 13, 2012·ACS Medicinal Chemistry Letters·H Bauke AlbadaNils Metzler-Nolte
Sep 4, 2016·FEMS Microbiology Reviews·Manuel Montalbán-LópezO P Kuipers
May 23, 2017·Natural Product Reports·P Klahn, M Brönstrup
Apr 21, 2019·Medicinal Research Reviews·Thanh-Nhat PhamPascal Sonnet
Dec 27, 2012·Nature Reviews. Microbiology·Paul D CotterColin Hill
Mar 3, 2019·Scientific Reports·Jarosław RuczyńskiIvan Kocić
Aug 24, 2017·Journal of Computer-aided Molecular Design·Zeynep KurkcuogluAlexandre M J J Bonvin
Jul 1, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Hannah L BoltSteven L Cobb
May 18, 2020·Applied Microbiology and Biotechnology·S A NavarroMiriam C Chalón
Jan 15, 2021·Comprehensive Reviews in Food Science and Food Safety·Yanlong CuiXin Lü

Related Concepts

Lipid II
Antibiotics
Drug Combinations
Fungus Drug Sensitivity Tests
Nisin
Uridine Diphosphate N-Acetylmuramic Acid
AB-Vancomycin
Enterococcus
Vancomycin Resistance
Antibiotics

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An antifungal, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis, cryptococcal meningitis, and others. Discover the latest research on antifungals here.