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Efflux Pumps and These Inhibitors
VNU Journal of Science: Medical and Pharmaceutical Sciences, 2019 In this era of multi-drug resistance, efflux pump is one of the major problems which is increasingly concerned by scientists. The structure and mechanism activity of the efflux pumps on both bacteria and eurakyotes that are gradually being clarified. Since then, efflux pump inhibitors have also been studied and initially applied in clinic, that makes ...
Le Minh Tri +6 more
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Antibiotics, 2023 One promising approach in treating antibiotic-resistant bacteria is to “break” resistances connected with antibacterial efflux by co-administering efflux pump inhibitors (EPIs) with antibiotics. Here, ten compounds, previously optimized to restore the susceptibility to ciprofloxacin (CIP) of norA-overexpressing Staphylococcus aureus, were evaluated for
Rampacci, Elisa +5 more
openaire +4 more sources
Mechanism Underlying the Reversal of Drug Resistance in P-Glycoprotein-Expressing Leukemia Cells by Pinoresinol and the Study of a Derivative [PDF]
, 2017 P-glycoprotein (P-gp) is a membrane protein associated with multidrug resistance (MDR) due to its key role in mediating the traffic of chemotherapeutic drugs outside cancer cells, leading to a cellular response that hinders efforts toward successful ...
Carpinella, Maria Cecilia +10 more
core +2 more sources
Synthesis of Berberine—Efflux Pump Inhibitor Hybrid Antibacterials [PDF]
Synthetic Communications, 2010 This paper reports the compact synthesis of two isomeric dual-action hybrid antimicrobials where the 13-position of the antibacterial berberine has been linked via 3'- and 4'-methylene bridges to INF55 (5-nitro-2-phenylindole), an inhibitor of the bacterial NorA multidrug-resistance pump.
Bremner, J. B., Kelso, Michael J
openaire +3 more sources
Molecular similarity of MDR inhibitors [PDF]
, 2004 Everyone is free to re-use the published material if proper accreditation/citation of the original publication is given. http://creativecommons.org/licences/by/3.0/The molecular similarity of multidrug resistance (MDR) inhibitors was evaluated using the ...
Gibbons, S., Zloh, Mire
core +2 more sources
Membranes, 2020 Resistance to antibiotics has made diseases that previously healed easily become more difficult to treat. Staphylococcus aureus is an important cause of hospital-acquired infections and multi-drug resistant.
Saulo R. Tintino +14 more
doaj +1 more source
A truncated AdeS kinase protein generated by ISAba1 insertion correlates with tigecycline resistance in Acinetobacter baumannii. [PDF]
PLoS ONE, 2012 Over-expression of AdeABC efflux pump stimulated continuously by the mutated AdeRS two component system has been found to result in antimicrobial resistance, even tigecycline (TGC) resistance, in multidrug-resistant Acinetobacter baumannii (MRAB ...
Jun-Ren Sun +8 more
doaj +1 more source
Not only P-glycoprotein: amplification of the ABCB1-containing chromosome region 7q21 confers multidrug resistance upon cancer cells by coordinated overexpression of an assortment of resistance-related proteins [PDF]
, 2017 The development of drug resistance continues to be a dominant hindrance toward curative cancer treatment. Overexpression of a wide-spectrum of ATP-dependent efflux pumps, and in particular of ABCB1 (P-glycoprotein or MDR1) is a well-known resistance ...
Assaraf, Yehuda G. +4 more
core +1 more source
Increased SK3 expression in DM1 lens cells leads to impaired growth through a greater calcium-induced fragility [PDF]
, 2006 Although cataract is a characteristic feature of myotonic dystrophy type 1 (DM1), little is known of the underlying mechanisms. We generated four lens epithelial cell lines derived from DM1 cataracts and two from age-matched, non-DM cataracts. Small-pool
Abe +40 more
core +2 more sources
Efflux pump inhibitors: targeting mycobacterial efflux systems to enhance TB therapy [PDF]
Journal of Antimicrobial Chemotherapy, 2015 The emergence of drug resistance continues to plague TB control, with a global increase in the prevalence of MDR-TB. This acts as a gateway to XDR-TB and thus emphasizes the urgency for drug development and optimal treatment options. Bedaquiline is the first new anti-TB drug approved by the FDA in 40 years and has been shown to be an effective ...
Caroline M, Pule +6 more
openaire +2 more sources