title: Macrolide antibiotics: binding site, mechanism of action, resistance.
abstract: Macrolides are among the most clinically important antibiotics. However, many aspects of macrolide action and resistance remain obscure. In this review we summarize the current knowledge, as well as unsolved questions, regarding the principles of macrolide binding to the large ribosomal subunit and the mechanism of drug action. Two mechanisms of macrolide resistance, inducible expression of Erm methyltransferase and peptide-mediated resistance, appear to depend on specific interactions between the ribosome-bound macrolide molecule and the nascent peptide. The similarity between these mechanisms and their relation to the general mode of macrolide action is discussed and the discrepancies between currently available data are highlighted.
authors.affiliation: Center for Pharmaceutical Biotechnology - M/C 870, University of Illinois, 900 S Ashland Ave, Chicago, IL 60607, USA.
authors.forename: Marne
authors.initials: M
authors.lastname: Gaynor
authors.forename: Alexander S
authors.initials: AS
authors.lastname: Mankin
mesh_terms: D000900:Anti-Bacterial Agents / Q000378:metabolism* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects* / Q000378:metabolism*; D001483:Base Sequence; D001665:Binding Sites / Q000187:drug effects; D024881:Drug Resistance, Bacterial; D018942:Macrolides; D008958:Models, Molecular; D008969:Molecular Sequence Data; D012270:Ribosomes / Q000187:drug effects / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D018942:Macrolides