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efflux pump inhibition

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https://www.readbyqxmd.com/read/28319068/iron-addiction-a-novel-therapeutic-target-in-ovarian-cancer
#1
D Basuli, L Tesfay, Z Deng, B Paul, Y Yamamoto, G Ning, W Xian, F McKeon, M Lynch, C P Crum, P Hegde, M Brewer, X Wang, L D Miller, N Dyment, F M Torti, S V Torti
Ovarian cancer is a lethal malignancy that has not seen a major therapeutic advance in over 30 years. We demonstrate that ovarian cancer exhibits a targetable alteration in iron metabolism. Ferroportin (FPN), the iron efflux pump, is decreased, and transferrin receptor (TFR1), the iron importer, is increased in tumor tissue from patients with high grade but not low grade serous ovarian cancer. A similar profile of decreased FPN and increased TFR1 is observed in a genetic model of ovarian cancer tumor-initiating cells (TICs)...
March 20, 2017: Oncogene
https://www.readbyqxmd.com/read/28314281/chemosensitizing-properties-of-%C3%AE-caryophyllene-and-%C3%AE-caryophyllene-oxide-in-combination-with-doxorubicin-in-human-cancer-cells
#2
Silvia DI Giacomo, Antonella DI Sotto, Gabriela Mazzanti, Michael Wink
BACKGROUND/AIM: The natural sesquiterpenes β-caryophyllene (CRY) and β-caryophyllene oxide (CRYO) were evaluated for their potential chemosensitizing properties. MATERIALS AND METHODS: CRY and CRYO cytotoxicity was tested against the Caco-2, CCRF/CEM and CEM/ADR5000 human cancer cell lines. Furthermore, combination experiments were carried out in order to study the ability of the sesquiterpenes to increase doxorubicin cytotoxicity. The possible interference of CRY and CRYO with functionality of ATP-binding cassette (ABC)-transporters was also investigated by Rhodamine123 efflux assay...
March 2017: Anticancer Research
https://www.readbyqxmd.com/read/28294992/new-roads-leading-to-old-destinations-efflux-pumps-as-targets-to-reverse-multidrug-resistance-in-bacteria
#3
REVIEW
Gabriella Spengler, Annamária Kincses, Márió Gajdács, Leonard Amaral
Multidrug resistance (MDR) has appeared in response to selective pressures resulting from the incorrect use of antibiotics and other antimicrobials. This inappropriate application and mismanagement of antibiotics have led to serious problems in the therapy of infectious diseases. Bacteria can develop resistance by various mechanisms and one of the most important factors resulting in MDR is efflux pump-mediated resistance. Because of the importance of the efflux-related multidrug resistance the development of new therapeutic approaches aiming to inhibit bacterial efflux pumps is a promising way to combat bacteria having over-expressed MDR efflux systems...
March 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28270804/eradication-and-sensitization-of-methicillin-resistant-staphylococcus-aureus-to-methicillin-with-bioactive-extracts-of-berry-pomace
#4
Serajus Salaheen, Mengfei Peng, Jungsoo Joo, Hironori Teramoto, Debabrata Biswas
The therapeutic roles of phenolic blueberry (Vaccinium corymbosum) and blackberry (Rubus fruticosus) pomace (commercial byproduct) extracts (BPE) and their mechanism of actions were evaluated against methicillin resistant Staphylococcus aureus (MRSA). Five major phenolic acids of BPE, e.g., protocatechuic, p. coumaric, vanillic, caffeic, and gallic acids, as well as crude BPE completely inhibited the growth of vegetative MRSA in vitro while BPE+methicillin significantly reduced MRSA biofilm formation on plastic surface...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28258237/computational-modelling-of-efflux-pumps-and-their-inhibitors
#5
REVIEW
Venkata Krishnan Ramaswamy, Pierpaolo Cacciotto, Giuliano Malloci, Attilio V Vargiu, Paolo Ruggerone
Antimicrobial resistance is based on the multifarious strategies that bacteria adopt to face antibiotic therapies, making it a key public health concern of our era. Among these strategies, efflux pumps (EPs) contribute significantly to increase the levels and profiles of resistance by expelling a broad range of unrelated compounds - buying time for the organisms to develop specific resistance. In Gram-negative bacteria, many of these chromosomally encoded transporters form multicomponent 'pumps' that span both inner and outer membranes and are driven energetically by a primary or secondary transporter component...
February 28, 2017: Essays in Biochemistry
https://www.readbyqxmd.com/read/28258236/the-role-played-by-drug-efflux-pumps-in-bacterial-multidrug-resistance
#6
REVIEW
Mohsen Chitsaz, Melissa H Brown
Antimicrobial resistance is a current major challenge in chemotherapy and infection control. The ability of bacterial and eukaryotic cells to recognize and pump toxic compounds from within the cell to the environment before they reach their targets is one of the important mechanisms contributing to this phenomenon. Drug efflux pumps are membrane transport proteins that require energy to export substrates and can be selective for a specific drug or poly-specific that can export multiple structurally diverse drug compounds...
February 28, 2017: Essays in Biochemistry
https://www.readbyqxmd.com/read/28243063/novel-5-oxo-hexahydroquinoline-derivatives-design-synthesis-in-vitro-p-glycoprotein-mediated-multidrug-resistance-reversal-profile-and-molecular-dynamics-simulation-study
#7
Omolbanin Shahraki, Najmeh Edraki, Mehdi Khoshneviszadeh, Farshid Zargari, Sara Ranjbar, Luciano Saso, Omidreza Firuzi, Ramin Miri
Overexpression of the efflux pump P-glycoprotein (P-gp) is one of the important mechanisms of multidrug resistance (MDR) in many tumor cells. In this study, 26 novel 5-oxo-hexahydroquinoline derivatives containing different nitrophenyl moieties at C4 and various carboxamide substituents at C3 were designed, synthesized and evaluated for their ability to inhibit P-gp by measuring the amount of rhodamine 123 (Rh123) accumulation in uterine sarcoma cells that overexpress P-gp (MES-SA/Dx5) using flow cytometry...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28238773/inhibition-of-the-tetk-efflux-pump-by-the-essential-oil-of-chenopodium-ambrosioides-l-and-%C3%AE-terpinene-against-staphylococcus-aureus-is-58
#8
Paulo W Limaverde, Fábia F Campina, Francisco A B da Cunha, Francidalva D Crispim, Fernando G Figueredo, Luciene F Lima, Cícera Datiane de M Oliveira-Tintino, Yedda M L S de Matos, Maria Flaviana B Morais-Braga, Irwin R A Menezes, Valdir Q Balbino, Henrique D M Coutinho, José P Siqueira-Júnior, Jackson R G S Almeida, Saulo R Tintino
The use of natural products is crucial to suppress the development of these micro-organisms and to reduce the concentration necessary to inhibit these microrganisms, reducing the toxicity risks also. In this study, the essential oil from Chenopodium ambrosioides Leaves and its main constituent α-Terpinene were used in the antibacterial and potentiating activity of antibiotics and ethidium bromide assays, against the bacterial strains Staphylococcus aureus IS-58, carriers of efflux pumps. The Minimum Inhibitory Concentration (MIC) was determined using a microdilution method...
February 23, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28231453/siderophore-transport-by-mmpl5-mmps5-protein-complex-in-mycobacterium-tuberculosis
#9
Padmani Sandhu, Yusuf Akhter
Iron is an essential metal ion required for the various physiological activities of bacteria. The pathogenic bacteria remain dependent on the host cell for their iron requirements and evolved with specialized scavenging machinery in the form of iron chelating siderophores. Mycobacterium tuberculosis has two types of siderophore molecules, mycobactin and carboxymycobactin. These are synthesized inside bacterial cells and need to be transported outside by specialized membrane associated proteins. MmpL5-MmpS5 (mycobacterial membrane protein large5-mycobacterial membrane protein small5) complex has been linked to the export of non-ferrated siderophores to extracellular environment but the precise molecular mechanism involved was largely unknown...
February 14, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28228097/alkaloid-extracts-from-combretum-zeyheri-inhibit-the-growth-of-mycobacterium-smegmatis
#10
Tafadzwa Nyambuya, Ruvimbo Mautsa, Stanley Mukanganyama
BACKGROUND: Current tuberculosis regimens have failed to combat the issue of drug resistance and ethno medicines may represent a possible source of antimycobacterial agents. Combretum species are well known in African traditional medicines and used for various ailments including pneumonia, venereal diseases like syphilis, mental problems, relief of sore throats and colds, fever, and chest coughs associated with tuberculosis. Alkaloids function as either hydrogen-acceptor or hydrogen-donor in hydrogen bonding critical for the interaction between targets thus, potentiating effects of curative agents on diseases...
February 23, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28219526/antifungal-activity-of-ionic-liquids-based-on-menthol-a-mechanism-study
#11
Jakub Suchodolski, Joanna Feder-Kubis, Anna Krasowska
The mechanism of toxicity of chiral ionic liquids with (1R,2S,5R)-(-)-menthol [Cn-Am-Men][Cl] (n=10, 11 or 12) in the fungus Candida albicans is reported here. Ionic liquids were more toxic towards Candida strain lacking all identified multidrug resistance efflux pumps. Moreover, the compounds tested inhibited C. albicans filamentation at the concentration at which detached fungal cells also adhered to the plastic surface. Our results showed the high activity of all the tested chiral ionic liquids in the permeabilization of C...
April 2017: Microbiological Research
https://www.readbyqxmd.com/read/28202577/nimesulide-and-4-hydroxynimesulide-as-bile-acid-transporters-inhibitors-are-contributory-factors-for-drug-induced-cholestasis
#12
Lei Zhou, Xiaoyan Pang, Jingfang Jiang, Dafang Zhong, Xiaoyan Chen
Nimesulide (NIM) is a classic nonsteroidal anti-inflammatory drug. However, some patients treated with NIM suffered from cholestatic liver injury. For this reason, we investigated the potential mechanism underlying NIM-induced cholestasis by using in vivo and in vitro models. Oral administration of 100 mg/kg/day NIM to Wistar rats for 5 days increased the levels of plasma total bile acids, alkaline phosphatase, alanine aminotransferase, and aspartate aminotransferase by 1.49-, 1.31-, 1.60-, and 1.29-fold, respectively...
February 15, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28173641/effects-of-adamantyl-derivatives-on-pharmacokinetic-behavior-of-paclitaxel-in-rats
#13
Kyung Mi Kim, Kyeong Lee, Kyusic Jang, Yae Seul Moon, Hwa Jeong Lee, Sandy Jeong Rhie
Paclitaxel (PTX) is one of the most frequently used anticancer agent for treating refractory ovarian cancer, metastatic breast cancer and non-small cell lung cancer. However, its oral administration is impeded by very low bioavailability (<5%) due to the P-glycopprotein (P-gp) efflux pump effect. This study investigated in vitro and in vivo P-gp inhibitory effects of adamantyl derivatives AC-603 and AC-786 in rats. Two adamantyl derivatives tested in this study increased the cytotoxicity of daunomycin (DNM) in P-gp overexpressed cell line by inhibiting P-gp efflux function...
February 6, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28169223/insights-into-the-ion-coupling-mechanism-in-the-mate-transporter-norm-vc
#14
Alexander Krah, Ulrich Zachariae
Bacteria have developed a variety of different mechanisms to defend themselves from compounds that are toxic to them, such as antibiotics. One of these defence mechanisms is the expulsion of drugs or other noxious compounds by multidrug efflux pumps. Multidrug and toxic compound extrusion (MATE) transporters are efflux pumps that extrude metabolic waste and a variety of antibiotics out of the cell, using an ion gradient as energy source. They function via an alternative-access mechanism. When ions bind in the outward facing conformation, a large conformational change to the inward facing conformation is induced, from which the ion is released and the extruded chemical compound is bound...
February 7, 2017: Physical Biology
https://www.readbyqxmd.com/read/28161596/polygoni-multiflori-radix-derived-anthraquinones-alter-bile-acid-disposition-in-sandwich-cultured-rat-hepatocytes
#15
Li Kang, Luqin Si, Jing Rao, Dan Li, Ya Wu, Sanlan Wu, Minghui Wu, Sijie He, Wenwen Zhu, Yang Wu, Jiaqiang Xu, Gao Li, Jiangeng Huang
Hepatic adverse reaction associated with Polygoni Multiflori Radix (PMR) has been frequently reported in recent years. Highly-enriched anthraquinones (AQs) in PMR, such as emodin, chrysophanol and physcion, have been found to be hepatotoxic. In the present study, sandwich-cultured rat hepatocytes (SCRHs) were employed to investigate the effect of individual and combined AQs on the disposition of endogenous bile acids (BAs) and exogenous probe substrates including deuterium-labeled taurocholate (d5-TCA), glycochenodeoxycholic acid (d4-GCDCA) and 5 (and 6)-carboxy-2',7'-dichlorofluorescein (CDF)...
February 2, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28160861/antibacterial-activity-of-epigallocatechin-3-gallate-egcg-and-its-synergism-with-%C3%AE-lactam-antibiotics-sensitizing-carbapenem-associated-multidrug-resistant-clinical-isolates-of-acinetobacter-baumannii
#16
Spencer Lee, Ghaida Saleh Al Razqan, Dong H Kwon
BACKGROUND: Infections caused by Acinetobacter baumannii were responsive to conventional antibiotic therapy. However, recently, carbapenem-associated multidrug resistant isolates have been reported worldwide and present a major therapeutic challenge. Epigallocatechin-3-Gallate (EGCG) extracted from green tea exhibits antibacterial activity. PURPOSE: We evaluated the antibacterial activity of EGCG and possible synergism with antibiotics in carbapenem-associated multidrug resistant A...
January 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28154323/exploration-of-molecular-targets-in-the-development-of-new-therapeutics-aimed-at-overcoming-multidrug-resistance
#17
Shozo Nishida, Masanobu Tsubaki
 Multidrug resistance (MDR) in cancer is a major problem in clinical settings: MDR correlates with a patient's poor prognosis and decreased quality of life. Recently, MDR was found to be involved in various signal pathways, so the inhibition of signal molecules by molecular targeting drugs may help overcome MDR. In addition, the acquisition of MDR is shown to be associated with the overexpression of drug efflux pumps such as P-glycoprotein (MDR1), which in turn affects the regulation of the expression of cell survival factors, B-cell leukemia protein 2 (Bcl-2) family proteins, etc...
2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/28153721/mir-138-indirectly-regulates-the-mdr1-promoter-by-nf-%C3%AE%C2%BAb-p65-silencing
#18
J L Requenez-Contreras, E S López-Castillejos, R Hernández-Flores, M A Moreno-Eutimio, J T Granados-Riveron, G U Martinez-Ruiz, G Aquino-Jarquin
MicroRNAs (miRNAs) are known to mediate post-transcriptional gene silencing in the cytoplasm and recent evidence indicates that may also possess nuclear roles in regulating gene expression. A previous study showed that miR-138 is involved in the multidrug resistance of leukemia cells through down-regulation of the drug efflux pump P-glycoprotein (P-gp), the protein encoded by the human multidrug-resistant ABCB1/MDR1 gene. However, the transcriptional regulatory mechanisms responsible remain to be elucidated...
March 11, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28146280/assessment-of-bile-salt-export-pump-bsep-inhibition-in-membrane-vesicles-using-radioactive-and-lc-ms-based-detection-methods
#19
Lisa D Marroquin, Paul D Bonin, Julie Keefer, Thomas Schroeter
The bile salt export pump (BSEP, ABCB11) belongs to the ATP-binding-cassette superfamily of transporters and is predominately found in the liver. BSEP is an efflux transporter that plays a critical role in the secretion of bile salts into the bile. Inhibition of BSEP function by drugs can result in the buildup of bile salts in the liver and eventually leads to cholestasis and drug-induced liver injury (DILI). DILI is a major cause of withdrawal of drugs from the pharmaceutical market and accounts for >50% of acute liver failures...
February 1, 2017: Current Protocols in Toxicology
https://www.readbyqxmd.com/read/28143610/severe-toxicity-induced-by-accumulation-of-active-sunitinib-metabolite-in-a-japanese-patient-with-renal-cell-carcinoma-a-case-report
#20
Shinya Takasaki, Masafumi Kikuchi, Yoshihide Kawasaki, Akihiro Ito, Yoichi Arai, Hiroaki Yamaguchi, Nariyasu Mano
BACKGROUND: Sunitinib is a multi-targeted tyrosine kinase inhibitor that is approved for treatment of renal cell carcinoma as an oral anticancer drug. Therapeutic drug monitoring of total sunitinib (sunitinib and N-desethyl sunitinib) is used in our hospital to improve therapeutic efficacy, while preventing adverse effects. Here, we report the first case of a patient with metastatic renal cell carcinoma undergoing hemodialysis and presenting severe adverse events induced by the accumulation of N-desethyl sunitinib...
February 1, 2017: Journal of Medical Case Reports
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