Frontiers in Medicinal Chemistry

Volume: 2

Indexed in: Scopus, EMBASE, Chemical Abstracts, EBSCO, Ulrich's Periodicals Directory.

Frontiers in Medicinal Chemistry is a book series devoted to the review of areas of important topical interest to medicinal chemists and others in allied disciplines. Frontiers in Medicinal Chemistry ...
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Macrolide Antibiotics: Binding Site, Mechanism of Action, Resistance

Pp. 21-35 (15)

Marne Gaynor and Alexander S. Mankin

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.

Keywords:

Macrolides, erythromycin, ketolides, azithromycin, clarithromycin, tylosin, carbomycin, spiramycin, ribosome, resistance

Affiliation:

Marne Gaynor, Alexander S. Mankin