Showing 1-29 of 29 results for "21882"
Priyamvada Chandra et al.
Drug metabolism and disposition: the biological fate of chemicals, 33(8), 1238-1243 (2005-05-24)
This study examined the impact of hepatic transport protein modulation on the hepatobiliary disposition of a nonmetabolized probe substrate, 5- (and 6)-carboxy-2',7'dichlorofluorescein (CDF) in rat isolated perfused livers (IPLs). In vivo treatment with modulators (100 and 200 mg/kg/day clofibric acid...
Amélie Moreau et al.
Fundamental & clinical pharmacology, 25(6), 743-752 (2011-01-08)
Macrophages represent major cellular targets of various drugs, especially antibiotics and anti-viral drugs. Factors that may govern intracellular accumulation of drugs in these cells, especially those related to activity of drug transporters, are consequently likely important to consider. The present...
Eliisa Mannermaa et al.
Pharmaceutical research, 26(7), 1785-1791 (2009-04-23)
The objective of this study was to characterize efflux proteins (P-glycoprotein (P-gp), multidrug resistance proteins (MRP1-6) and breast cancer resistance protein (BCRP)) of retinal pigment epithelium (RPE) cell lines. Expression of efflux proteins in two secondary (ARPE-19, D407) and two...
Christian Lechner et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 75(2), 284-290 (2010-03-24)
To establish a fluorescence-based assay for drug interactions with the ABC-export-protein MRP2 (ABCC2). Apical membrane vesicles were isolated by differential centrifugation from polarized MDCKII cells and MDCKII cells transfected with human MRP2. Vesicle fractions were characterized by electron microscopy, determination...
Vesna Munić et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 43(5), 359-369 (2011-05-25)
Based on our initial results on the effects of several ATP-binding cassette (ABC) transporter inhibitors on rhodamine-123 efflux from A549, a human lung carcinoma, and MES-SA, a human uterine sarcoma cell line, the aim of this study was to identify...
Cristobal L Miranda et al.
Chemical research in toxicology, 22(5), 863-874 (2009-03-31)
4-Hydroxy-2(E)-nonenal (HNE), a reactive aldehyde derived from oxidized lipids, has been implicated in the pathogenesis of cardiovascular and neurological diseases, in part by its ability to induce oxidative stress and by protein carbonylation in target cells. The effects of intracellular...
Heidi Kidron et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 46(1-2), 100-105 (2012-03-13)
MRP2 is an efflux transporter that is expressed mainly in the canalicular membrane of hepatocytes, where it expels polar and ionic compounds into the bile. MRP2 is also present in the apical membrane of enterocytes and epithelial cells of proximal...
Jannik Vindeløv et al.
Yeast (Chichester, England), 19(5), 429-439 (2002-03-29)
The effect of hyperosmotic shock on cell volume, vacuole volume, and intracellular pH (pH(i)) of individual cells of Saccharomyces cerevisiae and Zygosaccharomyces mellis was investigated. After transfer from a high water activity (a(w)) medium to low a(w) media, the growth...
Kati-Sisko Vellonen et al.
Journal of pharmaceutical sciences, 99(2), 1087-1098 (2009-07-23)
ATP-binding cassette (ABC) transporters are able to efflux their substrate drugs from the cells. We compared expression of efflux proteins in normal human corneal epithelial tissue, primary human corneal epithelial cells (HCEpiC), and corneal epithelial cell culture model (HCE model)...
Ken-Ichi Nezasa et al.
Drug metabolism and disposition: the biological fate of chemicals, 34(4), 718-723 (2006-01-26)
This study characterized the hepatobiliary disposition of 5 (and 6)-carboxy-2',7'-dichlorofluorescein (CDF), a model Abcc2/Mrp2 (canalicular) and Abcc3/Mrp3 (basolateral) substrate, in perfused livers from male C57BL/6 wild-type, Abcg2-/-, and Abcc2-/- mice. After single-pass liver perfusion with 1 muM CDF diacetate for...
Ekkehard Stehfest et al.
Archives of toxicology, 80(3), 125-133 (2005-12-24)
Defense against toxic endo- and xenobiotics is a major concern of all living species and ABC transporters play a vital role in this defense system. Multidrug resistance associated proteins 1 (MRP1) is a cellular detoxifying factor supposed to transport a...
Susan Pratt et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 27(5), 524-532 (2005-12-13)
Multidrug resistance protein-5 (MRP5, ABCC5) is a member of the ATP-binding cassette transporter superfamily that effluxes a broad range of natural and xenobiotic compounds such as cyclic GMP, antiviral compounds, and cancer chemotherapeutic agents including nucleoside-based drugs, antifolate agents and...
B Laupèze et al.
Life sciences, 68(11), 1323-1331 (2001-03-10)
Multidrug resistance proteins (MRPs) such as MRP1, MRP2 and MRP3 are membrane efflux pumps involved in multidrug resistance and handling organic anions. In the present study, MRP activity was investigated in normal mature leucocytes and CD34-positive hematopoietic cells from peripheral...
Yixian Liu et al.
Die Pharmazie, 73(9), 503-507 (2018-09-19)
The purpose of the present study was to dig into recent studies designed to characterize the impacts of 2'-deoxy-2'-β-fluoro-4'-azidocytidine (FNC) on P-glycoprotein (P-gp), multidrug resistance-associated protein 2 (MRP2) and breast cancer resistance protein (BCRP). Specifically, the modulation effects of FNC...
Phyllanthin and hypophyllanthin inhibit function of P-gp but not MRP2 in Caco-2 cells.
Sukhaphirom N, Vardhanabhuti N, et al.
J. Pharm. Pharm. Sci., 65, 292-299 (2013)
M Nedergaard et al.
Analytical biochemistry, 187(1), 109-114 (1990-05-15)
Derivatives of fluorescein sensitive to pH are extensively utilized for the determination of intracellular pH (pHi). Available dyes have pKa values of approximately 7.0, and are not well suited for measuring acidic pHi. We examined the fluorescein derivative, 5 (and...
A A Boldyrev
Bulletin of experimental biology and medicine, 140(1), 33-37 (2005-10-29)
Short-term incubation of lymphocytes with homocysteine or its oxidation product homocysteinic acid increased the formation of reactive oxygen species and cell necrosis (in case of homocysteinic acid). Effective concentration of homocysteine and homocysteinic acid (500 microM) significantly surpassed the level...
Takeo Nakanishi et al.
Toxicology and applied pharmacology, 263(2), 244-250 (2012-07-07)
We previously reported a quantitative time-lapse imaging (QTLI)-based analysis method to assess drug-drug interactions (DDI) at multidrug resistance-associated protein 2 (Mrp2) in rat sandwich-cultured hepatocyte (SCH) system, utilizing the fluorescent Mrp2 substrate, 5-(and 6)-carboxy-2',7'-dichlorofluorescein (CDF). Here, we aimed to examine...
Krisztina Heredi-Szabo et al.
Journal of biomolecular screening, 13(4), 295-301 (2008-03-20)
MRP2 (ABCC2) is an efflux transporter expressed on the apical membrane of polarized cells. This protein has a major role in the biliary elimination of toxic compounds from the liver. As MRP2 transports many endogenous compounds, including LTC4 as well...
L Payen et al.
Biochemical pharmacology, 60(12), 1967-1975 (2000-12-08)
Organic anion secretion by human hepatocytes was characterized using primary liver parenchymal cell cultures and the anionic fluorescent dye carboxy-2',7'-dichlorofluorescein (CF). Probenecid, a well-known common blocker of the membrane transport process for anions, was shown to increase CF accumulation in...
Sanna Siissalo et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 71(2), 332-338 (2008-09-09)
The aim of this work was to develop a screening method for MRP2 efflux substrates using the well-characterized, human-based intestinal Caco-2 cell model as a platform. MRP2 has a significant role in drug absorption and disposition and is known to...
Hsueh-Meei Huang et al.
Free radical biology & medicine, 37(11), 1779-1789 (2004-11-06)
Mitochondrial dysfunction and oxidative stress occur in neurodegenerative diseases. Other results show that bombesin-releasable calcium stores (BRCS) from the endoplasmic reticulum (ER) are exaggerated in fibroblasts from patients with Alzheimer's disease (AD) compared with controls and in fibroblasts from a...
Maciej J Zamek-Gliszczynski et al.
Drug metabolism and disposition: the biological fate of chemicals, 40(9), 1825-1833 (2012-06-20)
Transporter gene knockout rats are practically advantageous over murine models for pharmacokinetic and excretion studies, but their phenotypic characterization is lacking. At present, relevant aspects of pharmacokinetics, metabolism, distribution, and excretion of transporter probes [P-glycoprotein (P-gp): loperamide and paclitaxel; breast...
B Laupèze et al.
Human immunology, 62(10), 1073-1080 (2001-10-16)
P-glycoprotein (P-gp), an ATP-binding cassette (ABC) drug efflux pump, has been recently shown to play an important role in the physiology of Langherans cells, a subtype of dendritic cells (DC) found in the skin. The present study was designed to...
B Laupeze et al.
International journal of oncology, 15(3), 571-576 (1999-07-31)
Multidrug resistance-associated protein (MRP) and P-glycoprotein are drug efflux pumps conferring multidrug resistance to tumor cells and sharing numerous substrates. In order to determine a flow cytometric assay allowing to analyse MRP activity in cancerous cells in a sensitive and...
Federico Colombo et al.
Xenobiotica; the fate of foreign compounds in biological systems, 42(2), 157-163 (2011-10-04)
Prediction of biliary excretion is a challenge for drug discovery scientists due to the lack of in vitro assays. This study explores the possibility of establishing a simple assay to predict in vivo biliary excretion via the mrp2 transport system....
Katharine Howe et al.
Drug metabolism and disposition: the biological fate of chemicals, 37(2), 391-399 (2008-11-22)
The impact of transport proteins in the disposition of chemicals is becoming increasingly evident. Alteration in disposition can cause altered pharmacokinetic and pharmacodynamic parameters, potentially leading to reduced efficacy or overt toxicity. We have developed a quantitative in silico model...
Ridhi Parasrampuria et al.
Drug metabolism letters, 5(1), 64-72 (2011-01-05)
Rhodamine 123 (RH-123) and its glucuronidated metabolite (RH-Glu) are excreted into the bile via the ABC efflux transporters P-glycoprotein (P-gp) and multidrug resistance-related protein type 2 (Mrp2), respectively. In this study, we investigated the short-term (2 h) effects of a...
Jay E Mellon
Toxins, 7(8), 3257-3266 (2015-08-22)
Several atoxigenic Aspergillus flavus isolates, including some being used as biocontrol agents, and one toxigenic isolate were surveyed for the ability to produce extracellular xylanolytic and pectinolytic hydrolases. All of the tested isolates displayed good production of endoxylanases when grown...

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