Naslov
How do macrolide antibiotics interact with bacterial ribosomes?

Autori
Novak ; Predrag

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

Izvornik
Current Medicinal Chemistry / Rahman ; Atta-ur - Sharjah : Bentham Science, 2012, 102-102

Skup
4th International Conference on Drug Discovery & Therapy

Mjesto i datum
Dubai, Ujedinjeni Arapski Emirati, 12.02.2012. - 15.02.2012

Vrsta sudjelovanja
Pozvano predavanje

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
antibiotics; bacteria; macrolide; ribosomes

Sažetak
Macrolide antibiotics, such as azithromycin, have been widely prescribed for the treatment of respiratory tract infections owing to their high efficacy and safety. In spite of a number of existing macrolide antibiotics, the emerging multi-drug resistant microbial pathogens present serious and challenging problems which demand novel and more effective antimicrobial agents to be discovered. An effective approach to overcoming this problem is to understand the principles of how these drugs interact with their target ribosome. Recently available crystal structures of some ribosome-macrolide complexes have thrown new light on the binding mechanisms. However, when analysing solid state structures of ribosome-macrolide complexes one should keep in mind the discrepancies between obtained results. We believe that important steps in drug design should also include elucidation of the solution-state structures of free and bound macrolides since the structural features of the complex may not be exactly the same in solution and in the solid state. Here, a combination of NMR spectroscopy and molecular modeling is employed to determine free and bound conformations of macrolides and their binding epitopes in solution state. The knowledge gained from these studies will be discussed which can help in developing strategies aiming at design of potential inhibitors.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA