Molecular basis for inhibition of AcrB multidrug efflux pump by novel and powerful pyranopyridine derivatives
… 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 …
cell division (RND) exporters from Gram-negative bacteria. Overexpression of RND-type …
Optimization of a novel series of pyranopyridine RND efflux pump inhibitors
Z Aron, TJ Opperman - Current opinion in microbiology, 2016 - Elsevier
… characterization of the pyranopyridine (Pypy) MBX2319 (Figure 1) as an inhibitor of the
AcrAB efflux pump of E… activity relationships of the pyranopyridine efflux pump inhibitors. By …
AcrAB efflux pump of E… activity relationships of the pyranopyridine efflux pump inhibitors. By …
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 …
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…
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 …
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 …
the pyranopyridine MBX2319 (Figure 7). This compound is chemical derived and has potent …
[HTML][HTML] In vitro and in silico analysis of the efficiency of tetrahydropyridines as drug efflux inhibitors in Escherichia coli
…, LL Carrion, A von Groll, SS Costa, E Junqueira… - International journal of …, 2017 - Elsevier
… NUNL02 was found to be an AcrB efflux pump substrate. … The AcrAB–TolC system present
in Escherichia coli consists of … concentration than that of pyranopyridines MBX2319, MBX3132 …
in Escherichia coli consists of … concentration than that of pyranopyridines MBX2319, MBX3132 …
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 “…
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
… 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, …
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…
first described in 2014 by the US company MicroBiotix as AcrAB-TolC efflux pump inhibitors in E…