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PMID |
Sentence |
1 |
11159731
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The sulphonylurea glibenclamide inhibits multidrug resistance protein (MRP1) activity in human lung cancer cells.
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2 |
11159731
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In the present study, its effects towards multidrug resistance protein 1 (MRP1), an ABC efflux pump conferring multidrug resistance and handling organic anions, were investigated. 2.
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3 |
11159731
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Intracellular accumulation of calcein, an anionic dye substrate for MRP1, was strongly increased by glibenclamide in a dose-dependent manner in MRP1-overexpressing lung tumour GLC4/Sb30 cells through inhibition of MRP1-related calcein efflux.
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4 |
11159731
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Glibenclamide used at 12.5 microM was, moreover, found to strongly enhance the sensitivity of GLC4/Sb30 cells towards vincristine, an anticancer drug handled by MRP1. 4.
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5 |
11159731
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Efflux of carboxy-2',7'-dichlorofluorescein, an anionic dye handled by the ABC transporter MRP2 sharing numerous substrates with MRP1 and expressed at high levels in liver, was also strongly inhibited by glibenclamide in isolated rat hepatocytes. 5.
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6 |
11159731
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In summary, glibenclamide reversed MRP1-mediated drug resistance likely through inhibiting MRP1 activity and blocked organic anion efflux from MRP2-expressing hepatocytes.
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7 |
11159731
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The sulphonylurea glibenclamide inhibits multidrug resistance protein (MRP1) activity in human lung cancer cells.
|
8 |
11159731
|
In the present study, its effects towards multidrug resistance protein 1 (MRP1), an ABC efflux pump conferring multidrug resistance and handling organic anions, were investigated. 2.
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9 |
11159731
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Intracellular accumulation of calcein, an anionic dye substrate for MRP1, was strongly increased by glibenclamide in a dose-dependent manner in MRP1-overexpressing lung tumour GLC4/Sb30 cells through inhibition of MRP1-related calcein efflux.
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10 |
11159731
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Glibenclamide used at 12.5 microM was, moreover, found to strongly enhance the sensitivity of GLC4/Sb30 cells towards vincristine, an anticancer drug handled by MRP1. 4.
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11 |
11159731
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Efflux of carboxy-2',7'-dichlorofluorescein, an anionic dye handled by the ABC transporter MRP2 sharing numerous substrates with MRP1 and expressed at high levels in liver, was also strongly inhibited by glibenclamide in isolated rat hepatocytes. 5.
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12 |
11159731
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In summary, glibenclamide reversed MRP1-mediated drug resistance likely through inhibiting MRP1 activity and blocked organic anion efflux from MRP2-expressing hepatocytes.
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13 |
15070089
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Chemosensitivity assessed by collagen gel droplet embedded culture drug sensitivity test, and MDR1, MRP1, and MRP2 mRNA expression in human colorectal adenocarcinomas.
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14 |
16107775
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MDR1, MRP1 and MRP2 genotypes and in vitro chemosensitivity in Japanese patients with colorectal adenocarcinomas.
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15 |
16107775
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MMC was effective for those with a relatively high mRNA expression of the multidrug resistance-associated protein 2 (MRP2), whereas no correlation was found for the multidrug resistant transporter MDR1 and MRP1.
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16 |
16107775
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In this study, 3 genotypes of MDR1, 4 genotypes of MRP1, and 6 genotypes of MRP2 were additionally evaluated, and it was suggested that MDR1 C3435T and MRP2 G1249A were related with the susceptibility to colorectal adenocarcinoma.
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17 |
16107775
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The chemosensitivity against 5-FU, SN-38, MMC and CDDP was independent of MDR1 C3435T, MRP1 G2168A, and MRP2 C-24T (C3972T), possibly due to no association with the growth rate of and mRNA expression levels of MDR1, MRP1 and MRP2 in the adenocarcinoma, however, MDR1 C3435T tended to be accompanied with a higher expression of MDR1 mRNA.
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18 |
16107775
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MDR1, MRP1 and MRP2 genotypes and in vitro chemosensitivity in Japanese patients with colorectal adenocarcinomas.
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19 |
16107775
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MMC was effective for those with a relatively high mRNA expression of the multidrug resistance-associated protein 2 (MRP2), whereas no correlation was found for the multidrug resistant transporter MDR1 and MRP1.
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20 |
16107775
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In this study, 3 genotypes of MDR1, 4 genotypes of MRP1, and 6 genotypes of MRP2 were additionally evaluated, and it was suggested that MDR1 C3435T and MRP2 G1249A were related with the susceptibility to colorectal adenocarcinoma.
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21 |
16107775
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The chemosensitivity against 5-FU, SN-38, MMC and CDDP was independent of MDR1 C3435T, MRP1 G2168A, and MRP2 C-24T (C3972T), possibly due to no association with the growth rate of and mRNA expression levels of MDR1, MRP1 and MRP2 in the adenocarcinoma, however, MDR1 C3435T tended to be accompanied with a higher expression of MDR1 mRNA.
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22 |
17210751
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Regulation of human insulin, IGF-I, and multidrug resistance protein 2 promoter activity by hepatocyte nuclear factor (HNF)-1beta and HNF-1alpha and the abnormality of HNF-1beta mutants.
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23 |
17210751
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We analyzed the transactivity of wild-type and three mutant HNF-1beta on native human insulin, IGF-I, and multidrug resistance protein 2 (MRP2) promoters in combination with HNF-1alpha, using a reporter-assay system in transiently transfected mammalian cells.
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24 |
17210751
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In the human insulin gene promoter, we found that the cooperation of HNF-1alpha and HNF-1beta is prominent.
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25 |
17210751
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In the human IGF-I and MRP2 promoters, we found that the HNF-1beta His153Asn (H153N) mutant had a mutant-specific repressive effect on both HNF-1alpha and wild-type HNF-1beta transactivity.
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26 |
17210751
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Absence of the cooperation of HNF-1beta mutants with HNF-1alpha in the human insulin gene promoter might be one cause of defective insulin secretion.
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27 |
17210751
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The H153N mutant-specific repression of HNF-1alpha and HNF-1beta transactivity in human IGF-I and MRP2 promoters might explain the case-specific clinical features of growth retardation and cholestasis observed only in early infancy.
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28 |
17210751
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We found differential property of HNF-1alpha/HNF-1beta activity and the effect of HNF-1beta mutants by the promoters.
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29 |
17210751
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Regulation of human insulin, IGF-I, and multidrug resistance protein 2 promoter activity by hepatocyte nuclear factor (HNF)-1beta and HNF-1alpha and the abnormality of HNF-1beta mutants.
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30 |
17210751
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We analyzed the transactivity of wild-type and three mutant HNF-1beta on native human insulin, IGF-I, and multidrug resistance protein 2 (MRP2) promoters in combination with HNF-1alpha, using a reporter-assay system in transiently transfected mammalian cells.
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31 |
17210751
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In the human insulin gene promoter, we found that the cooperation of HNF-1alpha and HNF-1beta is prominent.
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32 |
17210751
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In the human IGF-I and MRP2 promoters, we found that the HNF-1beta His153Asn (H153N) mutant had a mutant-specific repressive effect on both HNF-1alpha and wild-type HNF-1beta transactivity.
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33 |
17210751
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Absence of the cooperation of HNF-1beta mutants with HNF-1alpha in the human insulin gene promoter might be one cause of defective insulin secretion.
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34 |
17210751
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The H153N mutant-specific repression of HNF-1alpha and HNF-1beta transactivity in human IGF-I and MRP2 promoters might explain the case-specific clinical features of growth retardation and cholestasis observed only in early infancy.
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35 |
17210751
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We found differential property of HNF-1alpha/HNF-1beta activity and the effect of HNF-1beta mutants by the promoters.
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36 |
17314201
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Transport of the dipeptidyl peptidase-4 inhibitor sitagliptin by human organic anion transporter 3, organic anion transporting polypeptide 4C1, and multidrug resistance P-glycoprotein.
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37 |
17314201
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In this report, we demonstrate that sitagliptin is transported by human organic anion transporter hOAT3 (Km=162 microM), organic anion transporting polypeptide OATP4C1, and multidrug resistance (MDR) P-glycoprotein (Pgp), but not by human organic cation transporter 2 hOCT2, hOAT1, oligopeptide transporter hPEPT1, OATP2B1, and the multidrug resistance proteins MRP2 and MRP4.
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38 |
17314201
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Our studies suggested that hOAT3, OATP4C1, and MDR1 Pgp might play a role in transporting sitagliptin into and out of renal proximal tubule cells, respectively.
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39 |
17314201
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Our data indicate that sitagliptin is unlikely to be a perpetrator of drug-drug interactions with Pgp, hOAT1, or hOAT3 substrates at clinically relevant concentrations.
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40 |
19728747
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The majority of currently used immunosuppressant drugs in organ transplantation are metabolized by cytochrome P450 (CYP) or uridine diphosphate-glucuronosyltransferases and are substrates of the multidrug resistance (MDR)-1 transporter P-glycoprotein, the MDR-associated protein 2 or the canalicular multispecific organic anion transporter, which predisposes these immunosuppressant compounds to specific interactions with commonly prescribed drugs.
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41 |
19937832
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In diabetic rats, Abcb1a, Abcc2, and Abcg2 (apical) were decreased, while Abcc4 (basolateral) was increased.
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42 |
22324395
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The aim of this study was to investigate effects of diabetes mellitus on function and expression of multidrug resistance-associated protein 2 (Mrp2) in rat liver, kidney and intestine.
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43 |
22324395
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Diabetes may enhance Mrp2 function and expression in liver, kidney and intestine, which might be due to insulin deficiency, increased TBA and conjugated bilirubin.
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44 |
22324395
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The aim of this study was to investigate effects of diabetes mellitus on function and expression of multidrug resistance-associated protein 2 (Mrp2) in rat liver, kidney and intestine.
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45 |
22324395
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Diabetes may enhance Mrp2 function and expression in liver, kidney and intestine, which might be due to insulin deficiency, increased TBA and conjugated bilirubin.
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46 |
22361279
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Rat Mrp2 gene expression is regulated by an interleukin-1β-stimulated biphasic response with enhanced transcription and subcellular shuttling of YB-1.
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47 |
22558111
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To determine if clinically important drug efflux transporter expression is altered in pregnancies complicated by gestational diabetes mellitus (GDM-I) or type 1 diabetes mellitus (T1DM-I), we compared the expression of multidrug resistance protein 1 (MDR1), multidrug resistance-associated protein 2 (MRP2) and the breast cancer resistance protein (BCRP) via western blotting and quantitative real-time polymerase chain reaction in samples obtained from insulin-managed diabetic pregnancies to healthy term-matched controls.
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48 |
22558111
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Significant changes in the placental protein expression of MDR1, MRP2, and BCRP were not detected (p>0.05).
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49 |
22558111
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Interestingly, there was a significant, positive correlation observed between plasma hemoglobin A1c levels (a retrospective marker of glycemic control) and both BCRP protein expression (r = 0.45, p<0.05) and BCRP mRNA expression (r = 0.58, p<0.01) in the insulin-managed DM groups.
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50 |
22558111
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Collectively, the data suggest that the expression of placental efflux transporters is not altered in pregnancies complicated by diabetes when hyperglycemia is managed; however, given the relationship between BCRP expression and plasma hemoglobin A1c levels it is plausible that their expression could change in poorly managed diabetes.
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