Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 3, Issue 9, Pages 949-960Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026033452159
Keywords
macrolides; erythromycin; ketolides; azithromycin; clarithromycin; tylosin; carbomycin; spiramycin; ribosome; resistance
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Funding
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R01GM053762] Funding Source: NIH RePORTER
- NIGMS NIH HHS [GM 53762] Funding Source: Medline
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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 Erin 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.
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