Novel DiOC3 96-well real-time efflux assay for discovery of NorA efflux pump inhibitors in Staphylococcus aureus

Elhidar, Najoua; Nafis, Ahmed; Göhler, André; Abbad, Abdelaziz; Hassani, Lahcen; Mezrioui, Nour-Eddine; Bohnert, Jürgen A.

doi:10.1016/j.mimet.2020.106128

Cited by 1 publication

(1 citation statement)

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“…One study optimised the method and established a novel DiOC 3 96-well real-time exclusion assay suitable for high-throughput efflux pump inhibitor screening using S. aureus . This approach does not use a potentially dangerous DNA insertion agent [ 88 ]. The use of virtual screening and physical experiments to complement and validate each other provides essential technical support to screen potentially valuable inhibitors.…”

Section: The Role Of Efflux Pump Inhibitors In Reversing Drug Resistancementioning

confidence: 99%

Bacterial Efflux Pump Inhibitors Reduce Antibiotic Resistance

Zhang,

Tian,

Sun

et al. 2024

Pharmaceutics

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Bacterial resistance is a growing problem worldwide, and the number of deaths due to drug resistance is increasing every year. We must pay great attention to bacterial resistance. Otherwise, we may go back to the pre-antibiotic era and have no drugs on which to rely. Bacterial resistance is the result of several causes, with efflux mechanisms widely recognised as a significant factor in the development of resistance to a variety of chemotherapeutic and antimicrobial medications. Efflux pump inhibitors, small molecules capable of restoring the effectiveness of existing antibiotics, are considered potential solutions to antibiotic resistance and have been an active area of research in recent years. This article provides a review of the efflux mechanisms of common clinical pathogenic bacteria and their efflux pump inhibitors and describes the effects of efflux pump inhibitors on biofilm formation, bacterial virulence, the formation of bacterial persister cells, the transfer of drug resistance among bacteria, and mismatch repair. Numerous efforts have been made in the past 20 years to find novel efflux pump inhibitors which are known to increase the effectiveness of medicines against multidrug-resistant strains. Therefore, the application of efflux pump inhibitors has excellent potential to address and reduce bacterial resistance.

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Section: The Role Of Efflux Pump Inhibitors In Reversing Drug Resistancementioning

confidence: 99%