Speakers:
- Helen Zgurskaya, George Lynn Cross Professor, University of Oklahoma (USA)
- Ruben Hartkoorn, Director of Research, Institut Pasteur de Lille (France)
- Timothy Opperman, Senior Research Scientist, Microbiotix (USA)
Moderator:
- Laura Piddock, Scientific Director, GARDP (Switzerland)
Presentation 1: Deciphering antibiotic resistance: Efflux pumps in bacteria (Helen Zgurskaya)
- Active efflux is the major mechanism of antibiotic resistance in Gram-negative pathogens.
- Efflux is synergistic with other mechanisms of resistance.
- Mechanistic studies identified transport intermediates for efficient inhibition of efflux.
- Efflux substrates, inhibitors and avoiders differ in molecular and physico-chemical properties.
Presentation 2: Discovery of efflux pump inhibitors effective against multi-drug resistant Gram-negative bacteria (Ruben Hartkoorn)
- Discovering a novel efflux pump inhibitor scaffold with a new mechanism of action
- Efflux pump inhibitor optimization and in vivo efficacy studies
Presentation 3: The hydrophobic trap (Timothy Opperman)
- Efflux pump inhibitors that bind to the hydrophobic trap or RND-type efflux pumps block conformational changes of the pump required to effectively extrude substrates, making this an important target for efflux pump inhibitors.
- The characteristics of a novel series of RND-type efflux pump inhibitors, the pyranopyridines, that bind to the “hydrophobic trap”, and the challenge of improving the drug-like properties of hydrophobic inhibitors will be presented.
This live webinar including an interactive Q&A session was broadcast on 23 April 2024.
If you have questions or comments, please let us know: revive@gardp.org.