Science · 1999 · 805 citations · 16 references
Life SciencesInfectious DiseasesMicrobiologyAntimicrobial ResistanceDrug DiscoveryMembrane BiochemistryAntibiotic ResistanceAntibiotic Resistance MechanismsAntimicrobial PeptidesBiological MembranesPeptide ChemistryPeptide Drug DiscoveryAntibacterial PeptidesAntimicrobial Peptide ActivityLipopeptide AntibioticsMembrane-active AntibioticsPeptide Structure-activity RelationshipsPore Formation MechanismsReceptorsVancomycin Resistance Mechanisms
Antibiotic resistance is rising, with high vancomycin resistance emerging in enterococci, and peptide antibiotics kill bacteria by permeabilizing membranes without specific receptors, acting in the micromolar range. The study shows that both vancomycin and the peptide nisin Z target the membrane‑anchored cell‑wall precursor Lipid II, with nisin’s high affinity and pore‑forming activity conferring nanomolar potency.
Resistance to antibiotics is increasing in some groups of clinically important pathogens. For instance, high vancomycin resistance has emerged in enterococci. Promising alternative antibiotics are the peptide antibiotics, abundant in host defense systems, which kill their targets by permeabilizing the plasma membrane. These peptides generally do not act via specific receptors and are active in the micromolar range. Here it is shown that vancomycin and the antibacterial peptide nisin Z use the same target: the membrane-anchored cell wall precursor Lipid II. Nisin combines high affinity for Lipid II with its pore-forming ability, thus causing the peptide to be highly active (in the nanomolar range).
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Emergence of vancomycin tolerance in Streptococcus pneumoniae
Robert W. Novak, Birgitta Henriques, Emmanuelle Charpentier et al. · Nature · 1999 · 352 citations
Structure of vancomycin and its complex with acetyl-D-alanyl-D-alanine
George M. Sheldrick, Peter G. Jones, Olga Kennard et al. · Nature · 1978 · 291 citations