engleski

Interactions of macrolides with their biological targets

Macrolide antibiotics are effective and well-tolerated therapeutic agents for treating infectious diseases owing to their high efficacy and safety. Macrolides bind to the ribosomal 23S rRNA in domain V at or near the peptidyl transferase region and block the exit tunnel through which the nascent peptides leave the ribosome. A crucial step in the discovery of novel compounds for preventing resistance is to understand the principles of how macrolides interact with their macromolecular targets. Hence, by applying one-and two-dimensional NMR experiments it is possible to characterise the interactions of macrolides and ribosomes and to determine the reactive groups responsible for binding. The two most commonly used NMR techniques to study macrolide binding are transferred nuclear Overhauser effect spectroscopy (trNOESY) and saturation transfer difference (STD) NMR experiments.

Macrolides ; interactions ; binding epitopes

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