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Pregled bibliografske jedinice broj: 985422

Unravelling Interactions of Macrolide Antibiotics ; What can NMR do?

Novak, Predrag
Unravelling Interactions of Macrolide Antibiotics ; What can NMR do? // NMRS 2018
Mohali, Indija, 2018. str. 32-32 (pozvano predavanje, međunarodna recenzija, sažetak, znanstveni)

Unravelling Interactions of Macrolide Antibiotics ; What can NMR do?

Novak, Predrag

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

NMRS 2018

Mjesto i datum
Mohali, Indija, 16.-19.02.2018

Vrsta sudjelovanja
Pozvano predavanje

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
NMR spectroscopy, Interactions, Macrolides

Macrolide antibiotics are effective therapeutic agents for treating infectious diseases owing to their high efficacy and safety. They inhibit bacterial protein biosynthesis by binding to the ribosomal 23S rRNA at the peptidyl transferase region and block the exit tunnel through which the nascent peptides leave the ribosome. In spite of a number of existing antibiotics, the emerging multi-drug resistant microbial pathogens present serious and challenging problems which demand novel and more potent antimicrobial agents to be discovered. An effective approach to overcoming this problem is to understand the principles of how these drugs interact with the ribosome. NMR spectroscopy is one of the most powerful and valuable methods in conformational analysis and structure-based inhibitor design. We have shown that an approach which combines one- and two-dimensional NMR methods and molecular modelling calculations could successfully be applied to conformational analysis of free and bound macrolides [1]. Furthermore, NOE based NMR techniques such as transferred NOE (tr-NOE) and saturation transfer difference (STD) provide further information on the bound state conformation and binding epitopes [2]. The application of NMR self-diffusion and solvent paramagnetic relaxation experiments can reveal the interaction strength and localization of macrolide antibiotics bound to their targets [3, 4]. In this talk the interactions of macrolides with ribosomes, membrane mimetics and bile acids will be presented and discussed.

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Autor s matičnim brojem:
Predrag Novak, (176404)