Nalazite se na CroRIS probnoj okolini. Ovdje evidentirani podaci neće biti pohranjeni u Informacijskom sustavu znanosti RH. Ako je ovo greška, CroRIS produkcijskoj okolini moguće je pristupi putem poveznice www.croris.hr
izvor podataka: crosbi !

Exploring macrolide binding modes by NMR spectroscopy (CROSBI ID 730008)

Prilog sa skupa u zborniku | sažetak izlaganja sa skupa | međunarodna recenzija

Novak, Predrag Exploring macrolide binding modes by NMR spectroscopy // CEUM 2022, Warsaw. 2022. str. 10-10

Podaci o odgovornosti

Novak, Predrag

engleski

Exploring macrolide binding modes by NMR spectroscopy

15- membered macrolides are well-known class of antibacterials widely prescribed to treat upper and lower respiratory tract infections 1. Azithromycin is a semi-synthetic macrolide antibiotic derived from erythromycin possessing broad spectrum of antibacterial potency and favorable pharmacokinetics. Similar to other macrolide antibiotics it exerts its activity by binding to the bacterial ribosomal 23S rRNA in domain V at the peptidyl transferase region and blocks the exit tunnel which in turn inhibits the bacterial protein synthesis. However, bacterial resistance to marketed antibiotics is growing rapidly and represents one of the major hazards to human health worldwide. Recently discovered conjugates of azithromycin and thiosemicarbazones, the macrozones, represent new class of macrolide derivatives that exhibit promising activities against resistant pathogens 2-3. Interaction studies of macrolide antibiotics and some selected macrozones with their biological targets will be presented in this talk. NMR experiments such as transferred nuclear Overhauser effect spectroscopy (trNOESY), saturation transfer difference (STD), diffusion and solvent paramagnetic relaxation experiments (PRE) in combination with molecular modelling have been employed to characterize binding modes and epitopes and asses bound conformations [4-6]. These data can serve as a platform for design of novel inhibitors with an improved biological profile.

macrolides, macrozones, interactions, binding modes, NMR spectroscopy

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

Podaci o prilogu

10-10.

2022.

objavljeno

Podaci o matičnoj publikaciji

CEUM 2022, Warsaw

Podaci o skupu

Central European NMR Symposium

ostalo

21.09.2022-23.09.2022

Varšava, Poljska

Povezanost rada

Kemija