Discovery of multidrug efflux pump inhibitors with a novel chemical scaffold

AT Green, M Moniruzzaman, CJ Cooper… - … et Biophysica Acta (BBA …, 2020 - Elsevier
… , inhibitors targeting both the efflux transporter AcrB and the membrane fusion protein AcrA in
the Escherichia coli AcrAB-TolC efflux pump … The pyranopyridine compound MBX2319 and …

[HTML][HTML] Optimization of pyridylpiperazine-based inhibitors of the Escherichia coli AcrAB-TolC efflux pump

…, JC Jiménez-Castellanos, V Meurillon, E Pradel… - European Journal of …, 2023 - Elsevier
… Several AcrAB-TolC efflux pump inhibitors (EPIs) have been … pyranopyridines of the MBX
series [[17], [18], [19], [20]]. We recently reported the discovery of a novel class of AcrB inhibitors

Comparative reassessment of AcrB efflux inhibitors reveals differential impact of specific pump mutations on the activity of potent compounds

S Schuster, M Vavra, DAN Wirth… - Microbiology Spectrum, 2024 - Am Soc Microbiol
… of the highly efficient pyranopyridine efflux pump inhibitors. Our … In Escherichia coli, the
trimeric efflux pump AcrB is complexed with … coli genome, only AcrAB-TolC reveals constitutive …

… approach to counter multidrug resistance in Gram-negative pathogens by targeting AcrB protein from AcrAB-TolC multidrug efflux pump from Escherichia coli

R Alenazy - Biology, 2022 - mdpi.com
… Another EPI that has been the subject of drug discovery efforts targeting AcrAB-TolC is
the pyranopyridine MBX2319 (Figure 7). This compound is chemical derived and has potent …

Analysis of orthogonal efflux and permeation properties of compounds leads to the discovery of new efflux pump inhibitors

M Moniruzzaman, CJ Cooper, MR Uddin… - ACS infectious …, 2022 - ACS Publications
… are present, for example, in the OM of Escherichia coli (E. coli) and other enterobacteria. (12,13) …
We next analyzed the ability of compounds to inhibit AcrAB-TolC-mediated efflux using …

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

…, JC Jiménez-Castellanos, RT Müller, E Pradel… - Nature …, 2022 - nature.com
… a novel chemical scaffold able to boost antibiotic activity in E. coli by inhibiting the AcrAB-TolC
efflux pump. In … Both the pyridopyrimidine and pyranopyridine inhibitors bind to a specific “…

Reserpine is the new addition into the repertoire of AcrB efflux pump inhibitors

A Shaheen, WA Afridi, S Mahboob, M Sana… - Molecular Biology, 2019 - Springer
… as those belonging to pyranopyridine, naphthamide and … Other examples of efflux pump
inhibitors from plant sources … to have efflux pump inhibitory activity against the Bmr efflux pump, …

Update on the discovery of efflux pump inhibitors against critical priority Gram-negative bacteria

N Compagne, A Vieira Da Cruz, RT Müller… - Antibiotics, 2023 - mdpi.com
… EPIs active against Escherichia coli or Pseudomonas aeruginosa. … Pyranopyridines were
first described in 2014 by the US company MicroBiotix as AcrAB-TolC efflux pump inhibitors in E

Characterization of pyridylpiperazine-based efflux pump inhibitors for Acinetobacter baumannii

JC Jiménez-Castellanos, E Pradel… - JAC-Antimicrobial …, 2023 - academic.oup.com
inhibit the Escherichia coli RND efflux pump AcrAB-TolC and boost the activity of several
antibiotics. Here we have evaluated and characterizedinhibition of the RND efflux pumps in A. …

Efflux pump inhibitors of clinically relevant multidrug resistant bacteria

A Lamut, L Peterlin Mašič, D Kikelj… - Medicinal Research …, 2019 - Wiley Online Library
… Staphylococcus aureus, AcrAB-TolC in Escherichia coli, and … and activity of AcrAB-TolC
efflux pump is associated with a … as well as interactions of pyranopyridine compounds in the …