Chlorpromazine and amitriptyline are substrates and inhibitors of the AcrB multidrug efflux pump

EM Grimsey, C Fais, RL Marshall, V Ricci, ML Ciusa… - MBio, 2020 - Am Soc Microbiol
Efflux is an important mechanism in Gram-negative bacteria conferring multidrug resistance.
Inhibition of efflux is an encouraging strategy to restore the antibacterial activity of antibiotics …

Molecular mechanism of MBX2319 inhibition of Escherichia coli AcrB multidrug efflux pump and comparison with other inhibitors

AV Vargiu, P Ruggerone, TJ Opperman… - Antimicrobial agents …, 2014 - Am Soc Microbiol
Efflux pumps of the resistance nodulation division (RND) superfamily, such as AcrB, make a
major contribution to multidrug resistance in Gram-negative bacteria. The development of …

Drug efflux pump inhibitors: a promising approach to counter multidrug resistance in Gram-negative pathogens by targeting AcrB protein from AcrAB-TolC multidrug …

R Alenazy - Biology, 2022 - mdpi.com
Simple Summary Multidrug-resistant bacterial infections, especially that caused by Gram-
negative bacteria, have posed serious health issues worldwide. Bacteria have different …

Molecular basis for inhibition of AcrB multidrug efflux pump by novel and powerful pyranopyridine derivatives

H Sjuts, AV Vargiu, SM Kwasny… - Proceedings of the …, 2016 - National Acad Sciences
The Escherichia coli AcrAB-TolC efflux pump is the archetype of the resistance nodulation
cell division (RND) exporters from Gram-negative bacteria. Overexpression of RND-type …

RND efflux pumps: structural information translated into function and inhibition mechanisms

P Ruggerone, S Murakami, KM Pos… - Current topics in …, 2013 - ingentaconnect.com
Efflux pumps of the Resistance Nodulation Division (RND) superfamily play a major role in
the intrinsic and acquired resistance of Gram-negative pathogens to antibiotics. Moreover …

Perturbed structural dynamics underlie inhibition and altered efflux of the multidrug resistance pump AcrB

E Reading, Z Ahdash, C Fais, V Ricci… - Nature …, 2020 - nature.com
Resistance–nodulation–division efflux pumps play a key role in inherent and evolved
multidrug resistance in bacteria. AcrB, a prototypical member of this protein family, extrudes …

Pyridylpiperazine-based allosteric inhibitors of RND-type multidrug efflux pumps

C Plé, HK Tam, A Vieira Da Cruz, N Compagne… - Nature …, 2022 - nature.com
Efflux transporters of the RND family confer resistance to multiple antibiotics in Gram-
negative bacteria. Here, we identify and chemically optimize pyridylpiperazine-based …

Discovery of multidrug efflux pump inhibitors with a novel chemical scaffold

AT Green, M Moniruzzaman, CJ Cooper… - … et Biophysica Acta (BBA …, 2020 - Elsevier
Multidrug efflux is a major contributor to antibiotic resistance in Gram-negative bacterial
pathogens. Inhibition of multidrug efflux pumps is a promising approach for reviving the …

[HTML][HTML] Molecular mechanisms of AcrB-mediated multidrug export

M Zwama, A Yamaguchi - Research in microbiology, 2018 - Elsevier
The over-expression of multidrug efflux pumps belonging to the Resistance-Nodulation-
Division (RND) superfamily is one of the main causes of multidrug-resistance (MDR) in …

Molecular insights into the determinants of substrate specificity and efflux inhibition of the RND efflux pumps AcrB and AdeB

J Wilhelm, KM Pos - Microbiology, 2024 - microbiologyresearch.org
Gram-negative bacterial members of the Resistance Nodulation and cell Division (RND)
superfamily form tripartite efflux pump systems that span the cell envelope. One of the …