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Advanced Methods for Studying Structure and Interactions of Macrolide Antibiotics

Department of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, HR-10000 Zagreb, Croatia
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Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(20), 7799; https://doi.org/10.3390/ijms21207799
Received: 20 September 2020 / Revised: 9 October 2020 / Accepted: 19 October 2020 / Published: 21 October 2020
Macrolide antibiotics are macrocyclic compounds that are clinically used and prescribed for the treatment of upper and lower respiratory tract infections. They inhibit the synthesis of bacterial proteins by reversible binding to the 23S rRNA at or near the peptidyl transferase center. However, their excellent antibacterial profile was largely compromised by the emergence of bacterial resistance. Today, fighting resistance to antibiotics is one of the greatest challenges in medicinal chemistry. Considering various physicochemical properties of macrolides, understanding their structure and interactions with macromolecular targets is crucial for the design of new antibiotics efficient against resistant pathogens. The solid-state structures of some macrolide-ribosome complexes have recently been solved, throwing new light on the macrolide binding mechanisms. On the other hand, a combination of NMR spectroscopy and molecular modeling calculations can be applied to study free and bound conformations in solution. In this article, a description of advanced physicochemical methods for elucidating the structure and interactions of macrolide antibiotics in solid state and solution will be provided, and their principal advantages and drawbacks will be discussed. View Full-Text
Keywords: structure characterization; macrolide antibiotics; macrolide interactions; biomolecular targets; X-ray crystallography; cryo-electron microscopy; NMR spectroscopy; biochemical and fluorescence methods; molecular dynamics simulations structure characterization; macrolide antibiotics; macrolide interactions; biomolecular targets; X-ray crystallography; cryo-electron microscopy; NMR spectroscopy; biochemical and fluorescence methods; molecular dynamics simulations
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MDPI and ACS Style

Jednačak, T.; Mikulandra, I.; Novak, P. Advanced Methods for Studying Structure and Interactions of Macrolide Antibiotics. Int. J. Mol. Sci. 2020, 21, 7799. https://doi.org/10.3390/ijms21207799

AMA Style

Jednačak T, Mikulandra I, Novak P. Advanced Methods for Studying Structure and Interactions of Macrolide Antibiotics. International Journal of Molecular Sciences. 2020; 21(20):7799. https://doi.org/10.3390/ijms21207799

Chicago/Turabian Style

Jednačak, Tomislav, Ivana Mikulandra, and Predrag Novak. 2020. "Advanced Methods for Studying Structure and Interactions of Macrolide Antibiotics" International Journal of Molecular Sciences 21, no. 20: 7799. https://doi.org/10.3390/ijms21207799

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