Albany 2019: 20th Conversation - Abstracts

category image Albany 2019
Conversation 20
June 11-15 2019
Adenine Press (2019)

Kinetic and Molecular Determinants of Antibiotic Permeation Barriers

The permeability barrier of Gram-negative cell envelopes is the major obstacle in the discovery and development of new antibiotics. In Gram-negative bacteria, these difficulties are exacerbated by the synergistic interaction between two biochemically distinct phenomena, the low permeability of the outer membrane and active multidrug efflux. We developed an approach to separate the contributions of the two mechanisms in the activities of antibiotics and applied it in the discovery of efflux pump inhibitors and analyses of structure-activity relationships for active efflux and outer membrane permeation in different Gram-negative pathogens. This presentation will be focused on species- and context-dependent interplays between active drug efflux and drug permeation and how they affect antibacterial activities of antibiotics, substrate specificities of efflux pumps and efflux inhibitors.

Helen I. Zgurskaya

University of Oklahoma
Department of Chemistry and Biochemistry
Norman, OK, 73019, USA

Email: elenaz@ou.edu