Naslov
NMR STRATEGIES FOR MACROLIDE ANTIBIOTICS INTERACTIONS

Autori
Novak, Predrag

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

Skup
CEUM 2014

Mjesto i datum
Zagreb, Hrvatska, 16.10.2014. - 17.10.2014

Vrsta sudjelovanja
Pozvano predavanje

Vrsta recenzije
Nije recenziran

Ključne riječi
Macrolide antibiotics; NMR methods; interactions

Sažetak
NMR spectroscopy has experienced a rapid growth and widespread applications in drug research and development. A variety of NMR techniques has been developed for structure-based inhibitor design studies and for establishing structure activity relationships. Macrolide antibiotics are therapeutically important class of compounds that are effective inhibitors of bacterial protein biosynthesis. Macrolide antibiotics bind to the large 50S ribosomal subunit at or near the peptidyl transferase center and block the elongation of the peptide chain. Understanding the mechanism by which macrolides exert their activity is crucial for the design of novel molecules possessing bioactivity. However, the increasing resistance to antibiotics has become a global problem and much effort is now directed toward new and more potent classes of drugs to overcome resistance mechanisms. An effective approach to solve this problem is to understand the principles of how the drugs interact with their biological targets. In this talk an NMR strategy to study macrolide interactions will be presented and discussed. It includes NOE based experiments such as saturation transfer difference (STD) spectroscopy which provides information on the bound state macrolide conformation and their binding epitopes. Furthermore, the application of paramagnetic relaxation enhancement (PRE) induced by an inert lanthanide complex can reveal the immersion depth of macrolide antibiotics bound to their biological targets. The obtained results can help in designing novel and more potent classes of antibiotics active against the resistant bacteria.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA