Multidrug efflux in gram-negative bacteria: Rationally modifying compounds to avoid efflux pumps

D Gurvic, U Zachariae - bioRxiv, 2023 - biorxiv.org
Gram-negative bacteria cause the majority of critically drug-resistant infections,
necessitating the rapid development of new drugs with Gram-negative activity. However …

A cell-based infection assay identifies efflux pump modulators that reduce bacterial intracellular load

AL Reens, AL Crooks, CC Su, TA Nagy… - PLoS …, 2018 - journals.plos.org
Bacterial efflux pumps transport small molecules from the cytoplasm or periplasm outside
the cell. Efflux pump activity is typically increased in multi-drug resistant (MDR) pathogens; …

Pyridylpiperazine efflux pump inhibitor boosts in vivo antibiotic efficacy against K. pneumoniae

A Vieira Da Cruz, JC Jiménez-Castellanos… - EMBO Molecular …, 2024 - embopress.org
Antimicrobial resistance is a global problem, rendering conventional treatments less
effective and requiring innovative strategies to combat this growing threat. The tripartite …

Efflux-mediated drug resistance in bacteria: an update

XZ Li, H Nikaido - Drugs, 2009 - Springer
Drug efflux pumps play a key role in drug resistance and also serve other functions in
bacteria. There has been a growing list of multidrug and drug-specific efflux pumps …

Inhibition of multidrug efflux pumps belonging to the major facilitator superfamily in bacterial pathogens

MF Varela, J Stephen, D Bharti, M Lekshmi, S Kumar - Biomedicines, 2023 - mdpi.com
Bacterial pathogens resistant to multiple structurally distinct antimicrobial agents are
causative agents of infectious disease, and they thus constitute a serious concern for public …

Multidrug efflux pumps and the two-faced janus of substrates and inhibitors

HI Zgurskaya, JK Walker, JM Parks… - Accounts of chemical …, 2021 - ACS Publications
Conspectus Antibiotics are miracle drugs that can cure infectious bacterial diseases.
However, their utility is challenged by antibiotic-resistant bacteria emerging in clinics and …

Efflux in Gram-negative bacteria: what are the latest opportunities for drug discovery?

T Gil-Gil, P Laborda, LE Ochoa-Sánchez… - Expert Opinion on …, 2023 - Taylor & Francis
Introduction The resistance-nodulation-division (RND) family is the most important group of
multidrug efflux pumps in Gram-negative bacteria. Their inhibition increases the …

Quinoline derivatives as promising inhibitors of antibiotic efflux pump in multidrug resistant Enterobacter aerogenes isolates

A Mahamoud, J Chevalier, A Davin-Regli… - Current drug …, 2006 - ingentaconnect.com
Efflux pumps protect the bacterial cell by expelling toxic compounds before they reach
intracellular targets. Because this mechanism actively contributes to the resistance of a …

Advances in the Discovery of Efflux Pump Inhibitors as Novel Potentiators to Control Antimicrobial-Resistant Pathogens

S Zhang, J Wang, J Ahn - Antibiotics, 2023 - mdpi.com
The excessive use of antibiotics has led to the emergence of multidrug-resistant (MDR)
pathogens in clinical settings and food-producing animals, posing significant challenges to …

Enhancement of Antibiotic Activity against Multidrug-Resistant Bacteria by the Efflux Pump Inhibitor 3,4-Dibromopyrrole-2,5-dione Isolated from a Pseudoalteromonas …

KE Whalen, KL Poulson-Ellestad… - Journal of natural …, 2015 - ACS Publications
Members of the resistance nodulation cell division (RND) of efflux pumps play essential
roles in multidrug resistance (MDR) in Gram-negative bacteria. Here, we describe the …