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.