Scalable and Chromatography-Free Synthesis of Efflux Pump Inhibitor Phenylalanine Arginine β-Naphthylamide for its Validation in Wild-Type Bacterial Strains.
Sign Up to like & getrecommendations! Published in 2023 at "ChemMedChem"
DOI: 10.1002/cmdc.202300128
Abstract: Phenylalanine arginine β-naphthylamine, or PAβN, is a C-terminus capped dipeptide discovered as an RND-type efflux pump inhibitor (EPI) in 1999. Since then, PAβN has become a standard tool compound in EPI research and development. Despite… read more here.
Keywords: synthesis; efflux pump; phenylalanine arginine; type bacterial ... See more keywords
Discovering interrelated natural mutations of efflux pump KmrA from Klebsiella pneumoniae that confer increased multidrug resistance
Sign Up to like & getrecommendations! Published in 2022 at "Protein Science"
DOI: 10.1002/pro.4323
Abstract: Klebsiella pneumoniae is a notorious pathogen that can cause multiorgan infections, which is difficult to treat mainly due to the widely distributed efflux pumps. Our previous research discovered the upregulation of efflux pump KmrA conferred… read more here.
Keywords: pneumoniae; klebsiella pneumoniae; natural mutations; resistance ... See more keywords
Changes in efflux pump activity of Clostridium beijerinckii throughout ABE fermentation
Sign Up to like & getrecommendations! Published in 2021 at "Applied Microbiology and Biotechnology"
DOI: 10.1007/s00253-020-11072-2
Abstract: Abstract Pumping toxic substances through a cytoplasmic membrane by protein transporters known as efflux pumps represents one bacterial mechanism involved in the stress response to the presence of toxic compounds. The active efflux might also… read more here.
Keywords: abe fermentation; efflux; pump activity; efflux pump ... See more keywords
The efflux pump inhibitor tetrandrine exhibits synergism with fluconazole or voriconazole against Candida parapsilosis
Sign Up to like & getrecommendations! Published in 2019 at "Molecular Biology Reports"
DOI: 10.1007/s11033-019-05020-1
Abstract: In the last two decades, with the wide use of azoles, antifungal resistance among Candida parapsilosis has considered a matter of concern worldwide. The aim of this study is to evaluate the antifungal potentials of… read more here.
Keywords: efflux pump; candida parapsilosis; pump inhibitor; synergism ... See more keywords
Molecular profiling of multidrug-resistant river water isolates: insights into resistance mechanism and potential inhibitors
Sign Up to like & getrecommendations! Published in 2019 at "Environmental Science and Pollution Research"
DOI: 10.1007/s11356-019-05738-2
Abstract: Polluted waters are an important reservoir for antibiotic resistance genes and multidrug-resistant bacteria. This report describes the microbial community, antibiotic resistance genes, and the genetic profile of extended spectrum β-lactamase strains isolated from rivers at,… read more here.
Keywords: efflux pump; river water; resistance; multidrug resistant ... See more keywords
Identification of Binding Sites for Efflux Pump Inhibitors of the AcrAB-TolC Component AcrA.
Sign Up to like & getrecommendations! Published in 2019 at "Biophysical journal"
DOI: 10.1016/j.bpj.2019.01.010
Abstract: The overexpression of multidrug efflux pumps is an important mechanism of clinical resistance in Gram-negative bacteria. Recently, four small molecules were discovered that inhibit efflux in Escherichia coli and interact with the AcrAB-TolC efflux pump… read more here.
Keywords: component acra; binding sites; acrab tolc; efflux pump ... See more keywords
Aminoguanidine hydrazones (AGH's) as modulators of norfloxacin resistance in Staphylococcus aureus that overexpress NorA efflux pump.
Sign Up to like & getrecommendations! Published in 2018 at "Chemico-biological interactions"
DOI: 10.1016/j.cbi.2017.12.009
Abstract: One of the promising fields for improving the effectiveness of antimicrobial agents is their combination with efflux pump inhibitors (EPIs), which besides expanding the use of existing antibiotics. The goal of this research was to… read more here.
Keywords: staphylococcus aureus; efflux pump; nora efflux; hydrazones agh ... See more keywords
Acute toxicity of selenate and selenite and their impacts on oxidative status, efflux pump activity, cellular and genetic parameters in earthworm Eisenia andrei.
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DOI: 10.1016/j.chemosphere.2018.08.095
Abstract: Selenium (Se) is an essential element for humans, animals, and certain lower plants, but can be toxic at high concentration. Even though Se is potentially toxic, little information is available about the effects of Se… read more here.
Keywords: acute toxicity; activity; pump activity; efflux pump ... See more keywords
Genome-wide survey of efflux pump-coding genes associated with Cronobacter survival, osmotic adaptation, and persistence
Sign Up to like & getrecommendations! Published in 2019 at "Current opinion in food science"
DOI: 10.1016/j.cofs.2018.11.005
Abstract: Microorganisms express various transmembrane complexes collectively known as efflux pumps that influence their survival under stressful growth conditions. Although efflux pumps are important in resistance to antibiotics, disinfectants, and preservatives, little information about their presence… read more here.
Keywords: efflux pump; survival; osmotic adaptation; pump ... See more keywords
N,N'-disubstituted cinnamamide derivatives potentiate ciprofloxacin activity against overexpressing NorA efflux pump Staphylococcus aureus 1199B strains.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.03.028
Abstract: A multi-step procedure has been described which afforded satisfactory yields of N,N'-disubstituted cinnamamides derived from N-Boc-protected amino acids (Boc-Gly, Boc-Val, Boc-Phe). The key step of this synthesis was a regioselective RedAl reduction of an amide… read more here.
Keywords: derivatives potentiate; efflux pump; pump; cinnamamide derivatives ... See more keywords
Repurposing bioactive aporphine alkaloids as efflux pump inhibitors.
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DOI: 10.1016/j.fitote.2019.104371
Abstract: Extrusion of drugs or drug-like compounds through bacterial efflux pumps is a serious health issue that leads to loss in drug efficacy. Combinatorial therapies of low-efficacy drugs with efflux pump inhibitors may help to restore… read more here.
Keywords: roemerine; pump inhibitors; efflux pump; bmra ... See more keywords