Macrolide Antibiotics: Binding Site, Mechanism of Action, Resistance

Author(s): Marne Gaynor, Alexander S. Mankin.

Journal Name: Current Topics in Medicinal Chemistry

Volume 3 , Issue 9 , 2003

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 peptidemediated 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

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Article Details

VOLUME: 3
ISSUE: 9
Year: 2003
Page: [949 - 960]
Pages: 12
DOI: 10.2174/1568026033452159
Price: $58

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