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https://www.readbyqxmd.com/read/27889879/plasmid-mediated-quinolone-resistance-in-enterobacteriaceae-a-systematic-review-with-a-focus-on-mediterranean-countries
#1
REVIEW
B Yanat, J-M Rodríguez-Martínez, A Touati
Quinolones are a family of synthetic broad-spectrum antimicrobial drugs. These molecules have been widely prescribed to treat various infectious diseases and have been classified into several generations based on their spectrum of activity. Quinolones inhibit bacterial DNA synthesis by interfering with the action of DNA gyrase and topoisomerase IV. Mutations in the genes encoding these targets are the most common mechanisms of high-level fluoroquinolone resistance. Moreover, three mechanisms for plasmid-mediated quinolone resistance (PMQR) have been discovered since 1998 and include Qnr proteins, the aminoglycoside acetyltransferase AAC(6')-Ib-cr, and plasmid-mediated efflux pumps QepA and OqxAB...
November 26, 2016: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/27879334/intrinsic-resistance-of-burkholderia-cepacia-complex-to-benzalkonium-chloride
#2
Youngbeom Ahn, Jeong Myeong Kim, Ohgew Kweon, Seong-Jae Kim, Richard C Jones, Kellie Woodling, Gonçalo Gamboa da Costa, John J LiPuma, David Hussong, Bernard S Marasa, Carl E Cerniglia
: Pharmaceutical products that are contaminated with Burkholderia cepacia complex (BCC) bacteria may pose serious consequences to vulnerable patients. Benzyldimethylalkylammonium chloride (BZK) cationic surfactants are extensively used in medical applications and have been implicated in the coselection of antimicrobial resistance. The ability of BCC to degrade BZK, tetradecyldimethylbenzylammonium chloride (C14BDMA-Cl), dodecyldimethylbenzylammonium chloride (C12BDMA-Cl), decyldimethylbenzylammonium chloride (C10BDMA-Cl), hexyldimethylbenzylammonium chloride, and benzyltrimethylammonium chloride was determined by incubation in 1/10-diluted tryptic soy broth (TSB) to determine if BCC bacteria have the ability to survive and inactivate these disinfectants...
November 22, 2016: MBio
https://www.readbyqxmd.com/read/27878697/nf%C3%AE%C2%BAbp65-transcription-factor-modulates-resistance-to-doxorubicin-through-abc-transporters-in-breast-cancer
#3
Kobra Velaei, Nasser Samadi, Sina Soltani, Balal Barazvan, Jafar Soleimani Rad
BACKGROUND: Shedding light on chemoresistance biology of breast cancer could contribute to enhance the clinical outcome. Intrinsic or acquired resistance to chemotherapy is a major problem in breast cancer treatment. METHODS AND MATERIALS: The NFκB pathway by siRNAP65 and JSH-23 as a translocational inhibitor of NFκBP65 in the doxorubicin-resistant MCF-7 (MCF-7/Dox) and MCF-7 cells was blocked. Then, the ABC transporter expression and function were assessed by real-time qRT-PCR and flow cytometry, respectively...
November 23, 2016: Breast Cancer: the Journal of the Japanese Breast Cancer Society
https://www.readbyqxmd.com/read/27872201/identification-of-chemical-compounds-that-inhibit-protein-synthesis-in-pseudomonas-aeruginosa
#4
Stephanie O Palmer, Yanmei Hu, Megan Keniry, James M Bullard
Four inhibitory compounds were identified using a poly-uridylic acid (polyU) mRNA-directed aminoacylation/translation (A/T) protein synthesis system composed of phenylalanyl-tRNA synthetases (PheRS), ribosomes, and ribosomal factors from Pseudomonas aeruginosa in an in vitro screen of a synthetic compound library. The compounds were specific for inhibition of bacterial protein synthesis. In enzymatic assays, the compounds inhibited protein synthesis with IC50 values ranging from 20 to 60 μM. Minimum inhibitory concentrations (MICs) were determined in cultures for a panel of pathogenic organisms, including Enterococcus faecalis, Escherichia coli, Haemophilus influenzae, P...
November 21, 2016: Journal of Biomolecular Screening
https://www.readbyqxmd.com/read/27871991/tumor-targeted-micelle-forming-block-copolymers-for-overcoming-of-multidrug-resistance
#5
Alena Braunová, Libor Kostka, Ladislav Sivák, Lucie Cuchalová, Zuzana Hvězdová, Richard Laga, Sergey Filippov, Peter Černoch, Michal Pechar, Olga Janoušková, Milada Šírová, Tomáš Etrych
New amphiphilic diblock polymer nanotherapeutics serving simultaneously as a drug delivery system and an inhibitor of multidrug resistance were designed, synthesized, and evaluated for their physico-chemical and biological characteristics. The amphiphilic character of the diblock polymer, containing a hydrophilic block based on the N-(2-hydroxypropyl)methacrylamide copolymer and a hydrophobic poly(propylene oxide) block (PPO), caused self-assembly into polymer micelles with an increased hydrodynamic radius (Rh of approximately 15nm) in aqueous solutions...
November 18, 2016: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/27869748/design-of-new-antibacterial-enhancers-based-on-acrb-s-structure-and-the-evaluation-of-their-antibacterial-enhancement-activity
#6
Yi Song, Rongxin Qin, Xichun Pan, Qin Ouyang, Tianyu Liu, Zhaoxia Zhai, Yingchun Chen, Bin Li, Hong Zhou
Previously, artesunate (AS) and dihydroartemisinine 7 (DHA7) were found to have antibacterial enhancement activity against Escherichia coli via inhibition of the efflux pump AcrB. However, they were only effective against E. coli standard strains. This study aimed to develop effective antibacterial enhancers based on the previous work. Our results demonstrate that 86 new antibacterial enhancers were designed via 3D-SAR and molecular docking. Among them, DHA27 had the best antibacterial enhancement activity...
November 18, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27855620/mrp1-dependent-collateral-sensitivity-of-multidrug-resistant-cancer-cells-identifying-selective-modulators-inducing-cellular-glutathione-depletion
#7
Doriane Lorendeau, Lauriane Dury, Rachad Nasr, Ahcène Boumendjel, Elisabetta Teodori, Michael Gütschow, Pierre Falson, Attilio Di Pietro, Hélène Baubichon-Cortay
Cancer cells are permanently being selected for survival and proliferation. During this process, tumor cells often co-opt basic physiological mechanisms to protect themselves from toxic chemotherapy. One of these mechanisms is the overexpression of ATP-binding cassette (ABC) drug efflux pumps leading to multidrug resistance (MDR) of cancer cells through an increase of drug efflux. In the past 20 years, many efforts were done to circumvent MDR through the inhibition of ABC transporters. A number of inhibitors of these transporters were found but are rarely specific or rationally developed...
November 18, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27834897/curcumin-as-a-modulator-of-p-glycoprotein-in-cancer-challenges-and-perspectives
#8
REVIEW
Vanessa Lopes-Rodrigues, Emília Sousa, M Helena Vasconcelos
Multidrug resistance (MDR) presents a serious challenge to the efficiency of cancer treatment, and may be associated with the overexpression of drug efflux pumps. P-glycoprotein (P-gp) is a drug efflux pump often found overexpressed in cases of acquired MDR. Nevertheless, there are no P-gp inhibitors being used in the current clinical practice, due to toxicity problems, drug interactions, or pharmacokinetic issues. Therefore, it is important to identify novel inhibitors of P-gp activity or expression. Curcumin is a secondary metabolite isolated from the turmeric of Curcuma longa L...
November 10, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/27830269/inhibition-of-the-multidrug-efflux-pump-lmrs-from-staphylococcus-aureus-by-cumin-spice-cuminum-cyminum
#9
Prathusha Kakarla, Jared Floyd, MunMun Mukherjee, Amith R Devireddy, Madhuri A Inupakutika, Indrika Ranweera, Ranjana Kc, Ugina 'Shrestha, Upender Rao Cheeti, Thomas Mark Willmon, Jaclyn Adams, Merissa Bruns, Shravan Kumar Gunda, Manuel F Varela
Staphylococcus aureus is a serious causative agent of infectious disease. Multidrug-resistant strains like methicillin-resistant S. aureus compromise treatment efficacy, causing significant morbidity and mortality. Active efflux represents a major antimicrobial resistance mechanism. The proton-driven multidrug efflux pump, LmrS, actively exports structurally distinct antimicrobials. To circumvent resistance and restore clinical efficacy of antibiotics, efflux pump inhibitors are necessary, and natural edible spices like cumin are potential candidates...
November 9, 2016: Archives of Microbiology
https://www.readbyqxmd.com/read/27825482/unraveling-genomic-and-phenotypic-nature-of-multidrug-resistant-mdr-pseudomonas-aeruginosa-vrfpa04-isolated-from-keratitis-patient
#10
Murugan N, Malathi J, Umashankar V, Madhavan H N
Multidrug-resistant (MDR) Pseudomonas aeruginosa VRFPA04, obtained from a keratitis patient was found to exhibit resistance to betalactam (Penicillins, cephalosporins, including carbapenems, except aztreonam), aminoglycosides, quinolone group of drugs and susceptible to colistin. The complete genome sequencing of the ocular isolate to measure and ascertain the degree of multidrug resistance in VRFPA04 strain resulted in 6,818,030bp (6.8Mb) genome sizes, which happen to be the third largest genome available in the Genbank to date...
December 2016: Microbiological Research
https://www.readbyqxmd.com/read/27821447/synthetic-organotellurium-compounds-sensitize-drug-resistant-candida-albicans-clinical-isolates-to-fluconazole
#11
L F Reis de Sá, F T Toledo, A C Gonçalves, B A Sousa, A A Dos Santos, P F Brasil, V A Duarte da Silva, A C Tessis, J A Ramos, M A Carvalho, E Lamping, A Ferreira-Pereira
Invasive Candida albicans infections are a serious health threat for immunocompromised individuals. Fluconazole is most commonly used to treat these infections, but resistance due to the overexpression of multidrug efflux pumps is of grave concern. This study evaluated the ability of five synthetic organotellurium compounds to reverse fluconazole resistance of C. albicans clinical isolates. Compounds 1-4, at < 10 μg/ml, ameliorated fluconazole resistance of Saccharomyces cerevisiae strains overexpressing the major C...
November 7, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27816681/use-of-juglone-as-antibacterial-and-potential-efflux-pump-inhibitors-in-staphylococcus-aureus-isolated-from-the-oral-cavity
#12
Tarek Zmantar, Hanene Miladi, Bochra Kouidhi, Yassine Chaabouni, Rihab Ben Slama, Amina Bakhrouf, Kacem Mahdouani, Kamel Chaieb
In this study the minimal inhibitory concentration (MICs) of tetracycline (Tet), erythromycin (Ery) and benzalkonium chloride (BC) in absence and in presence of a sub-MIC of juglone (Jug) were determined. In addition, the Ethidium bromide (EtBr) efflux assay was performed to assess the effect of Jug on EtBr cells accumulation. Our results showed a selective antimicrobial activity of Jug against the tested strains. A synergistic effect of Jug, drugs (Tet and Ery) and disinfectant (BC) was noticed with a reduction rate varied from 2 to 16-fold...
November 2, 2016: Microbial Pathogenesis
https://www.readbyqxmd.com/read/27816545/effect-of-abemaciclib-ly2835219-on-enhancement-of-chemotherapeutic-agents-in-abcb1-and-abcg2-overexpressing-cells-in-vitro-and-in-vivo
#13
Tong Wu, Zhen Chen, Kenneth K W To, Xiaona Fang, Fang Wang, Bin Cheng, Liwu Fu
Multidrug resistance (MDR) is the major obstacle of the success in cancer chemotherapy. The overexpression of ATP-binding cassette (ABC) transporters, particularly ABCB1 and ABCG2, play a significant role in mediating MDR by pumping anticancer drugs out of cancer cells. Abemaciclib (LY2835219) is an orally bioavailable CDK4/6 inhibitor under phase III clinical trials. Here, we found that LY2835219 remarkably enhanced the efficacy of chemotherapeutic drugs in ABCB1 or ABCG2 over-expressing cancer cells in vitro and in vivo...
November 2, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27815466/fluorinated-beta-diketo-phosphorus-ylides-are-novel-efflux-pump-inhibitors-in-bacteria
#14
Annamária Kincses, Ágnes Míra Szabó, Ryosuke Saijo, Genki Watanabe, Masami Kawase, Joseph Molnár, Gabriella Spengler
BACKGROUND: One of the most important resistance mechanisms in bacteria is the increased expression of multidrug efflux pumps. To combat efflux-related resistance, the development of new efflux pump inhibitors is essential. MATERIALS AND METHODS: Ten phosphorus ylides were compared based on their MDR-reverting activity in multidrug efflux pump system consisting of the subunits acridine-resistance proteins A and B (AcrA and AcrB) and the multidrug efflux pump outer membrane factor TolC (TolC) of Escherichia coli K-12 AG100 strain and its AcrAB-TolC-deleted strain...
November 2016: In Vivo
https://www.readbyqxmd.com/read/27810576/effects-of-pharmaceuticals-and-personal-care-products-ppcps-on-multixenobiotic-resistance-mxr-related-efflux-transporter-activity-in-zebrafish-danio-rerio-embryos
#15
V Cunha, K Burkhardt-Medicke, P Wellner, M M Santos, P Moradas-Ferreira, T Luckenbach, M Ferreira
Certain ATP binding cassette (ABC) transporter proteins, such as zebrafish Abcb4, are efflux pumps acting as a cellular defence against a wide range of different, potentially toxic chemical compounds thus mediating so called multixenobiotic resistance (MXR). Certain chemicals target MXR proteins and, as so called chemosensitisers, inhibit the activity of these proteins thus increasing the toxicity of other chemicals that would normally be effluxed. In this study 14 pharmaceuticals and personal care products (PPCPs) that are being increasingly detected in aquatic systems, were assessed for interference with the MXR system of zebrafish (Danio rerio)...
October 28, 2016: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/27807430/resistance-to-biocides-in-listeria-monocytogenes-collected-in-meat-processing-environments
#16
Daniele Conficoni, Carmen Losasso, Enzo Cortini, Andrea Di Cesare, Veronica Cibin, Valerio Giaccone, Gianluca Corno, Antonia Ricci
The emergence of microorganisms exerting resistance to biocides is a challenge to meat-processing environments. Bacteria can be intrinsically resistant to biocides but resistance can also be acquired by adaptation to their sub-lethal concentrations. Moreover, the presence of biocide resistance determinants, which is closely linked to antibiotic resistance determinants, could lead to co-selection during disinfection practices along the food chain, and select cross-resistant foodborne pathogens. The purpose of this work was to test the resistance of wild strains of Listeria monocytogenes, isolated from pork meat processing plants, toward benzalkonium chloride (BC), used as proxy of quaternary ammonium compounds...
2016: Frontiers in Microbiology
https://www.readbyqxmd.com/read/27796140/in-vitro-and-in-vivo-evaluation-of-paclitaxel-lapatinib-loaded-f127-pluronic-micelles
#17
Pouya Dehghankelishadi, Ebrahim Saadat, Fatemeh Ravar, Maliheh Safavi, Mahboobeh Pordeli, Mehdi Gholami, Farid A Dorkoosh
The aim of this study was to evaluate the in vitro and in vivo efficacy of Paclitaxel-Lapatinib loaded Pluronic micelles. Lapatinib and pluronic sensitize the cancerous cells to Paclitaxel via efflux pump inhibition. In addition, pluronic polymers can trigger intrinsic apoptosis pathways. Furthermore, micellar system can passively target the chemotherapeutic agents by enhanced permeability and retention effect. The paclitaxel-lapatinib loaded micelles were characterized in means of encapsulation efficacy and size...
October 31, 2016: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/27793887/identification-of-important-compounds-isolated-from-natural-sources-that-have-activity-against-multidrug-resistant-cancer-cell-lines-effects-on-proliferation-apoptotic-mechanism-and-the-efflux-pump-responsible-for-multi-resistance-phenotype
#18
REVIEW
Leonard Amaral, Gabriella Spengler, Joseph Molnar
The focus of this mini-review is to identify non-toxic compounds isolated from natural sources (plants) that exhibit specific activity against efflux pumps of specific multidrug-resistant (MDR) cancer cell lines, inhibit proliferation of the MDR cancer cell lines and inhibit the activity of overexpressed efflux pumps of the MDR cancer cell line.
November 2016: Anticancer Research
https://www.readbyqxmd.com/read/27786239/simultaneous-delivery-of-paclitaxel-and-bcl-2-sirna-via-ph-sensitive-liposomal-nanocarrier-for-the-synergistic-treatment-of-melanoma
#19
Teegala Lakshminarayan Reddy, Koteswara Rao Garikapati, S Gopal Reddy, B V Subba Reddy, J S Yadav, Utpal Bhadra, Manika Pal Bhadra
pH-sensitive drug carriers that are sensitive to the acidic (pH = ~6.5) microenvironments of tumor tissues have been primarily used as effective drug/gene/siRNA/microRNA carriers for releasing their payloads to tumor cells/tissues. Resistance to various drugs has become a big hurdle in systemic chemotherapy in cancer. Therefore delivery of chemotherapeutic agents and siRNA's targeting anti apoptotic genes possess advantages to overcome the efflux pump mediated and anti apoptosis-related drug resistance...
October 27, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27768847/reviving-antibiotics-efflux-pump-inhibitors-that-interact-with-acra-a-membrane-fusion-protein-of-the-acrab-tolc-multidrug-efflux-pump
#20
Narges Abdali, Jerry M Parks, Keith M Haynes, Julie L Chaney, Adam T Green, David Wolloscheck, John K Walker, Valentin V Rybenkov, Jerome Baudry, Jeremy C Smith, Helen I Zgurskaya
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 reduce bacterial virulence. Identification of new druggable sites for inhibition is critical for the development of effective EPIs, especially in light of constantly emerging resistance. Here, we describe EPIs that interact with periplasmic membrane fusion proteins, critical components of efflux pumps that are responsible for the activation of the transporter and the recruitment of the outer-membrane channel...
November 2, 2016: ACS Infectious Diseases
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