Naslov
Epitope mapping of a macrozone interaction with ribosome by NMR spectroscopy and molecular modeling

Autori
Mikulandra, Ivana ; Škevin, Sonja ; Lulić, Ana- Marija ; Habinovec, Iva ; Jednačak, Tomislav ; Bertoša, Branimir ; Novak, Predrag

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

Izvornik
Adriatic NMR Conference 2019 : Book of abstracts / Namjesnik, Danijel ; Novak, Predrag ; Parlov Vuković, Jelena - Zagreb, 2019, 57-57

ISBN
978-953-6076-56-7

Skup
Adriatic NMR 2019

Mjesto i datum
Mali Ston, Hrvatska, 06.06.2019. - 09.06.2019

Vrsta sudjelovanja
Poster

Vrsta recenzije
Nije recenziran

Ključne riječi
macrolide antibiotics, conformations, epitope mapping, STD, trNOESY

Sažetak
Macrolide antibiotics, such as azithromycin have been widely used to treat infections of both gram- positive and gram-negative bacteria. They exert their biological activity by binding to bacterial ribosome at or near the peptidyl transferase center thus inhibiting protein biosynthesis. Emerging multi-drug resistant microbial pathogens present today a serious and challenging problem in medical treatment which demands novel antimicrobial agents to be obtained. In order to discover and design more effective macrolide compounds, it is important to explore the interactions with ribosome and other biological targets and to elucidate and characterize bound conformations in solution. We have prepared a series of bioactive azithromycin conjugates, the macrozones, by coupling thiosemicarbazones to azithromycin. Here we present results of interaction studies of a selected macrozone and ribosome isolated from E. Coli. We used a combination of NMR experiments such as transferred nuclear Overhauser effect spectroscopy (trNOESY) and saturation transfer difference (STD) and molecular modeling to characterize binding epitopes and asses bound conformations.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA