Bacterial efflux pump inhibitors

BJ Kamicker, MT Sweeney, F Kaczmarek… - New Antibiotic …, 2008 - Springer
Infections caused by multidrug-resistant Gram-negative pathogens play a major role in the
morbidity and mortality of hospitalized patients. The rise of resistance to current antibiotic …

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 …

Extending the Potency and Lifespan of Antibiotics: Inhibitors of Gram-Negative Bacterial Efflux Pumps

M Duffey, RP Jumde, RMA da Costa… - ACS Infectious …, 2024 - ACS Publications
Efflux is a natural process found in all prokaryotic and eukaryotic cells that removes a
diverse range of substrates from inside to outside. Many antibiotics are substrates of …

Recent advances toward a molecular mechanism of efflux pump inhibition

TJ Opperman, ST Nguyen - Frontiers in microbiology, 2015 - frontiersin.org
Multidrug resistance (MDR) in Gram-negative pathogens, such as the Enterobacteriaceae
and Pseudomonas aeruginosa, poses a significant threat to our ability to effectively treat …

Inhibition of bacterial efflux pumps: a new strategy to combat increasing antimicrobial agent resistance

GW Kaatz - Expert Opinion on Emerging Drugs, 2002 - Taylor & Francis
Resistance to multiple drugs in medically important bacteria results in therapeutic
challenges for the clinician. The mechanisms by which bacteria evade the effects of …

Ever-adapting RND efflux pumps in gram-negative multidrug-resistant pathogens: a race against time

M Zwama, K Nishino - Antibiotics, 2021 - mdpi.com
The rise in multidrug resistance (MDR) is one of the greatest threats to human health
worldwide. MDR in bacterial pathogens is a major challenge in healthcare, as bacterial …

Natural and synthetic compounds such as trimethoprim behave as inhibitors of efflux in Gram-negative bacteria

LJV Piddock, MI Garvey, MM Rahman… - Journal of …, 2010 - academic.oup.com
Objectives We hypothesized that small heterocyclic or nitrogen-containing compounds could
act as RND efflux pump inhibitors (EPIs). To ascertain possible EPIs, we sought to identify …

The development of efflux pump inhibitors to treat Gram-negative infections

P Blanco, F Sanz-García… - Expert opinion on …, 2018 - Taylor & Francis
Introduction: One of the possibilities for reducing the emergence and spread of antibiotic
resistance is the use of anti-resistance compounds capable of resensitizing resistant …

Efflux pumps: their role in antibacterial drug discovery

O Lomovskaya, WJ Watkins - Current medicinal chemistry, 2001 - ingentaconnect.com
The emergence of active efflux as a major causative factor in antibiotic resistance has been
one of the most significant trends in antiinfective chemotherapy over the last decade. The …

Can efflux inhibitors really counter resistance?

K Poole, O Lomovskaya - Drug Discovery Today: Therapeutic Strategies, 2006 - Elsevier
Efflux, particularly that mediated by the resistance-nodulation-division (RND) family of
multiple antibiotic efflux systems that are prevalent in Gram-negative pathogenic bacteria, is …