Expression of specific short peptides can render cells resistant to macrolide antibiotics. Peptides conferring resistance to structurally different macrolides including oleandomycin, azithromycin, azaerythromycin, josamycin and a ketolide cethromycin were selected from a random pentapeptide expression library. Analysis of the entire collection of the resistance peptides allowed their classifica...

significantly by long-term and low-dose treatment of 14memberedring macrolide antibiotics such as erythromycin (EM), clarithromycin (CAM) and roxithromycin (RXM)3'4). Anti-inflammatory mechanisms of macrolide antibiotics include the down-regulation of inflammatory cytokines and lymphocytes. EM and azithromycin (AZM), a 15memberedring macrolide antibiotic that has clinical effect in the treatmen...

The potentiation of the antiviral activity of acyclovir [9-[(2-hydroxyethoxy)methyl]guanine] by polyene macrolide antibiotics has been studied as a function of the macrolide structure. The 12 polyenes chosen for this study represented the major structural groups of these antibiotics and induced in mammalian cells repairable membrane alterations or irreversible cell damage. The potentiating acti...

The glycan portion of macrolide antibiotics modulates their efficacy. High-level expression of three macrolide GTs and kinetic analysis has revealed a highly selective synthetic "tool kit" with such plasticity that 12 glycan-modified macrolide antibiotics have been readily created. One of these (1-Gal) is enhanced over its parent oleandomycin (1) by "glycotargeting", allowing higher uptake thro...

The article provides an overview of current publications on the chemical structure, mechanism action and safety macrolide antibiotics. We conducted a search in PubMed Google Scholar databases for scientific articles published from 2010 to 2021. following key words were used: macrolides, antibiotics, erythromycin, clarithromycin, azithromycin, action, adverse drug reactions, toxicity. Macrolides...

Macrolide antibiotics bind in the nascent peptide exit tunnel of the ribosome and inhibit protein synthesis. The majority of information on the principles of binding and action of these antibiotics comes from studies that employed model organisms. However, there is a growing understanding that the binding of macrolides to their target, as well as the mode of inhibition of translation, can be st...

Structure of a novel antibiotic, sporeamicin A (SRM-A), was determined by a combination of spectroscopic and X-ray crystallographic studies. SRM-A has a unique structure containing a 2,3-dihydro-3-oxofuran moiety as part of a 14-membered macrolide ring.

Pattee, P. A. (Iowa State University, Ames) and J. N. Baldwin. Transduction of resistance to some macrolide antibiotics in Staphylococcus aureus. J. Bacteriol. 84:1049-1055. 1962.-By use of phage 80 of the International Typing Series, propagated on appropriate strains of Staphylococcus aureus, two related markers controlling resistance to certain macrolide antibiotics (erythromycin, oleandomyci...

Since 1950, well over fifty macrolides have been derived from various Actinomycetes in screening laboratories located at many corners of the world. Among the most intensely studied macrolides are those produced on a commercial scale (erythromycin, oleandomycin, tylosin, leucomycin and spiramycin) as well as examples of particular historical/scientific importance (Magnamycin, pikromycin, narbomy...

Many clinically effective therapeutic agents can exhibit localized and systemic effects that are manifestly different from their intended primary pharmacological mode of action. Macrolide antibiotics such as erythromycin and its derivatives are no exception. In addition to their antibacterial action, this class of antibiotics exhibits anti-inflammatory activity in a variety of airway diseases s...