Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 26 for “"MRP2"”.
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Multidrug resistance-associated protein 2 (MRP2) and oxaliplatin transport
… transporter multidrug resistance protein-2 (MRP2), encoded for by the ABCC2 gene, may play a role in determining cellular sensitivity to oxaliplatin by transporting oxaliplatin-derived platinum. Human MRP2-expressing inside-out membrane vesicles prepared from Sf9 insect cells were used for …
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Auswirkungen der obstruktiven Cholestase auf die intestinale Expression von MRP2 bei Ratten und Menschen
Multidrug resistance-associated protein 2 (MRP2), a transporter of organic anions in hepatocytes, renal epithelial cells, and enterocytes, is differentially regulated in liver and kidney during cholestasis, but little is known about its regulation in the intestine. We investigated duodenal protein …
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Structural and Functional Analysis of Substrate Recognition and Inhibition of the Multidrug Transporters MRP1 and MRP2
… hydrolysis, but also inhibits the activity of MRP2 (Chapter 4). To begin to understand the mechanism of CPI1 cross-inhibition of MRP2, I solve the structure of MRP2 in a ligand-free state. Unlike previously resolved structures of MRP1, the ligand-free structure of MRP2 features a segment of its …
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Age-Associated Hepatic Drug Transporter Expression and Its Implications for Pediatric Pharmacotherapyflexibility affect DNA topoisomerase I function
… and the multidrug resistance protein 2 (MRP2), serve as major hepatic transporters that mediate the biliary excretion of various organic anions and cations along with glutathione-, glucuronate-, or sulfate-conjugates of several drug substrates. However, very little is known about the …
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Isolierte Gehirn-Kapillaren als in vitro-Modell der Blut-Hirn Schranke
… der ABC-Transporter-Proteine P-Glykoprotein und Mrp2 auf den Transport von Arzneistoffen an der Blut-Hirn Schranke untersuchen kann. Es wurde untersucht, ob frisch isolierte Kapillaren aus dem Gehirn von Schweinen für diese Fragestellung geeignet sind, da bisher bekannte und verwendete Modelle …
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Einfluss von Tensiden auf die Resorption von Substraten der ABC-Transportproteine
… der aktiven Transportproteine, p-gp und MRP2 festgestellt. Dies stellt auch das größte Problem der Standardisierung des Modells dar. 2. Einfluss von Tensiden auf die Resorption von Arzneistoffen: Zahlreiche Arzneistoffe haben eine schlechte Bioverfügbarkeit, weil ihre intestinale …
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Molecular and Functional Analyses of Transport Proteins for Organic Anions
… transport mediated by the export proteins Mrp2 and Mrp4. In contrast to transport of the Mrp2-substrate fluorescein-methotrexate (FL-MTX), transport is not regulated by proteinkinase (PK) A, and PKC. For better characterization of kinetic parameters I studied transport of fluo-cAMP in …
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Pharmakokinetik von Doxorubicin: Populationsvariabilität und Einfluss von genetischen Polymorphismen in Membran-Trasportproteinen
… in den Membran-Transportproteinen MDR1, MRP1, MRP2, MRP3 und BCRP auf die Pharmakokinetik und ausgewählte Nebenwirkungen des Zytostatikums Doxorubicin zu untersuchen. Dazu wurden die Plasmakonzentrationen von Doxorubicin und Doxorubicinol von 94 Krebspatienten durch HPLC analysiert. Die …
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The Development of Methods to Account for Physiologic Dynamic Changes and Their Effects on the Pharmacokinetics of Therapeutic Monoclonal Antibodies and other Therapeutics
… on the dynamic changes in the ontogeny of MRP2 (an apical liver transport protein) and the dynamic changes caused by an immune response to a therapeutic monoclonal antibody (mAb). Several approaches can be used to limit or capture the changes in the pharmacokinetics of a medication caused …
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Prodrug Approach to Improve Oral and Brain Absorption of HIV Protease Inhibitor, Lopinavir
… solubility, intestinal efflux by P-gp and MRP2 and extensive hepatic metabolism (CYP3A4 enzymes). Furthermore, brain LPV absorption is poor due to high efflux by P-gp and MRP2 at blood-brain barrier (BBB), plasma protein binding (99%) and extensive CYP3A4 metabolism. Hence, to improve oral …
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Novel drug interaction for improving intracellular accumulation and efficacy of chemotherapeutics in retinoblastoma and mitochondrial localization of transporters in corneal epithelial cells
… resistant (MDR) efflux proteins (MDR1 and MRP2) over-expressed on retinoblastoma tumor. Ocular cells have shown good tolerability against antimicrobial moxifloxacin (fourth generation fluoroquinolone) at higher dose level. As majority of fluoroquinolones become ineffective due to efflux …
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Differentielle Regulation organischer Anionentransporter der Oatp-Familie bei Ethinylöstradiol-induzierter Cholestase der Ratte
… pump (Bsep) und multidrug resistance protein 2 (Mrp2) were analyzed after 0.5, 1,3 and 5 days of ethinylestradiol treatment (5mg/kg) in rats. Regulation in mRNA and Protein levels were determined by northern and westernblotting. Binding activities of Oatp2 and Ntcp transactivators were assessed …
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Untersuchung der Genexpression von ABC- und SLC-Transmembranproteinen mit Beteiligung am aktiven Transport von Antigenen, Eikosanoiden und Zytostatika beim malignen Melanom
… basic expression levels were detected for MRP1, MRP2, MRP4, OATP3A1 and the still functionally uncharacterized OATP5A1. We could also show a down-regulation of TAP1. TAP1 mediates antigen presentation via MHC-I. MRP can confer drug resistance by decreasing the intracellular drug concentration. …
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Transporter-Targeted Prodrug Delivery to Improve Oral Bioavailability of Saquinavir
… lowered cytotoxicity, and reduced P-gp/MRP2-mediated efflux activities regardless of stereochemistry in promoieties. SQV attached with L-isomers shows higher affinity for peptide transporters but lower stability and higher toxicity, whereas conjugation with D-isomers can enhance …
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Regulation of Human Renal Drug Transporters by Inflammatory Cytokines and Pregnancy-related Hormones in Primary Proximal Tubular Epithelial Cells
… and OAT3. GCDCA-S was transported by OAT3 and MRP2, and atenolol was transported by OCT2 and MATE1/2-K. Selective inhibitor combinations (e.g., nicotinic acid + quercetin for OAT2, GCDCA-S + cyclosporine A for OAT3, atenolol + mitoxantrone for OCT2) were identified to disentangle overlapping …
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In vitro Zellkulturmodelle der Blut-Hirn-Schranke zur Untersuchung der Permeation und P-Glycoprotein-Interaktion von Arzneistoffen
… der Zellen. Immunfärbungen des ABC-Transporters Mrp2 waren negativ. Die Ex-pression von P-Glycoprotein konnte dagegen nachgewiesen werden. Die Charakterisierung des in vitro Permeationsmodells der Blut-Hirn-Schranke erfolgte an-hand von Permeationsversuchen. Aufgrund der Untersuchungen wurden …
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Comparison of Redox-Active and Conjugative Enzymes With and Without Efflux Transporters and Their Comparative Effectiveness in Protection Against Cellular Toxicity of 4-Hydroxy-2-Nonenal (HNE), an Aldehyde Lipid Peroxidation Production
… including multi-drug resistance proteins (MRP1/MRP2) may be required for removal of HNE-SG. The combined role of GSTs with MRP1/2 was studied in stably transfected MCF7 and a HepG2 cell line model. Co-expression of GSTM1 + MRP1 leads to increased HNE-protein adducts formation and sensitization …
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Multidrug resistance proteins (MRP) transport the cytokine/nuclear protein High Mobility Group Box 1 (HMGB1) across membranes
… to ABC C group. Overexpression of MRP1/ABCC1, MRP2/ABCC2 and MRP3/ABCC3 endows activated cells with the ability to secrete HMGB 1. Moreover, macrophages from Mrp1-1- mice have impaired HMGB1 exocytosis. I also suggest that HMGB1 is unfolded during its translocation. MRP transporters are known …
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