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 …
pathogens. Inhibition of multidrug efflux pumps is a promising approach for reviving the …
Identification and Structure–Activity Relationships of Novel Compounds that Potentiate the Activities of Antibiotics in Escherichia coli
KM Haynes, N Abdali, V Jhawar… - Journal of medicinal …, 2017 - ACS Publications
In Gram-negative bacteria, efflux pumps are able to prevent effective cellular concentrations
from being achieved for a number of antibiotics. Small molecule adjuvants that act as efflux …
from being achieved for a number of antibiotics. Small molecule adjuvants that act as efflux …
Chlorpromazine and amitriptyline are substrates and inhibitors of the AcrB multidrug efflux pump
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 …
Inhibition of efflux is an encouraging strategy to restore the antibacterial activity of antibiotics …
Mechanistic duality of bacterial efflux substrates and inhibitors: example of simple substituted cinnamoyl and naphthyl amides
N D'Cunha, M Moniruzzaman, K Haynes… - ACS infectious …, 2021 - ACS Publications
Antibiotic resistance poses an immediate and growing threat to human health. Multidrug
efflux pumps are promising targets for overcoming antibiotic resistance with small-molecule …
efflux pumps are promising targets for overcoming antibiotic resistance with small-molecule …
Molecular mechanism of MBX2319 inhibition of Escherichia coli AcrB multidrug efflux pump and comparison with other inhibitors
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 …
major contribution to multidrug resistance in Gram-negative bacteria. The development of …
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
Optimization of compound permeation into Gram-negative bacteria is one of the most
challenging tasks in the development of antibacterial agents. Two permeability barriers─ …
challenging tasks in the development of antibacterial agents. Two permeability barriers─ …
Efflux pump inhibitors of clinically relevant multidrug resistant bacteria
A Lamut, L Peterlin Mašič, D Kikelj… - Medicinal Research …, 2019 - Wiley Online Library
Bacterial infections are an increasingly serious issue worldwide. The inability of existing
therapies to treat multidrug‐resistant pathogens has been recognized as an important …
therapies to treat multidrug‐resistant pathogens has been recognized as an important …
Reviving antibiotics: efflux pump inhibitors that interact with AcrA, a membrane fusion protein of the AcrAB-TolC multidrug efflux pump
Antibiotic resistance is a major threat to human welfare. Inhibitors of multidrug efflux pumps
(EPIs) are promising alternative therapeutics that could revive activities of antibiotics and …
(EPIs) are promising alternative therapeutics that could revive activities of antibiotics and …
Sequential mechanism of assembly of multidrug efflux pump AcrAB-TolC
EB Tikhonova, Y Yamada, HI Zgurskaya - Chemistry & biology, 2011 - cell.com
Multidrug efflux pumps adversely affect both the clinical effectiveness of existing antibiotics
and the discovery process to find new ones. In this study, we reconstituted and characterized …
and the discovery process to find new ones. In this study, we reconstituted and characterized …
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 …