INT130295
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Sentences Mentioned In
Key: | Protein | Mutation | Event | Anatomy | Negation | Speculation | Pain term | Disease term |
The present study further characterizes the expression of multidrug resistance-associated proteins 1-4 (Mrp1-4), breast cancer resistance protein (Bcrp) and sodium-taurocholate co-transporting polypeptide (Ntcp) in mouse liver following administration of the hepatotoxicants acetaminophen (APAP) and carbon tetrachloride (CCl4). | |||||||||||||||
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Alternatively, upregulation of the efflux transporter ABCG2 protein expression has been associated with MTX resistance in cancer cells [45], but no associations with SNPs evaluated in FPGS and clinical effects of MTX have been observed [44]. | |||||||||||||||
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This resistance is mediated by many mechanisms including over-expression of proteins involved in inhibition of apoptosis (i.e, Bcl-2), leading to insensitivity of tumor cells to apoptotic stimuli; an up-regulation of DNA repair; alteration of the target; up-regulation of detoxification enzymes (i.e., Glutathione S-transferases); and extrusion of chemotherapeutic drugs by overexpression of ATP-binding cassette family proteins, such as MRP (multidrug resistant-associated protein) BCRP (breast cancer resistance protein or mitoxantrone resistance protein) because these proteins regulate absorption, distribution, and excretion of various pharmacologic compounds [141]. | |||||||||||||||
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Real-time semiquantitative RT-PCR showed that lens epithelial SP cells express higher levels of ABCG2 than non-SP cells. | |||||||||||||||
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In vitro studies have revealed that the cellular response to folate deprivation is associated with increased expression of FPGS and decreased expression of ABCG2 [35], suggesting that the adaptive cellular response to low folate involves increased polyglutamation to promote the retention of folate. | |||||||||||||||
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One important feature of CSCs is their resistance to the cytotoxicity of varous chemotherapeutic agents because of their relatively high expression levels of multiple drug resistance transporters such as ABCB1 (MDR1/PGP, P-glycoprotein) and ABCG2 (MXR/BCRP) [38]. | |||||||||||||||
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Protein expression of Bcrp was unchanged with treatment. | |||||||||||||||
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Immunostaining of liver sections obtained 48 h after hepatotoxicant treatment confirmed expression patterns of a subset of transporters (Bcrp, Ntcp, Mrp3, and Mrp4). | |||||||||||||||
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One important feature of CSCs is their resistance to the cytotoxicity of varous chemotherapeutic agents because of their relatively high expression levels of multiple drug resistance transporters such as ABCB1 (MDR1/PGP, P-glycoprotein) and ABCG2 (MXR/BCRP) [38]. | |||||||||||||||
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This is the reason why BCRP mediated resistance to imatinib is attenuated by imatinib induced reduction of BCRP expression (Nakanishi et al 2006).
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SP cells expressed approximately 4.5-fold higher mRNA levels of the stem cell marker ABCG2 compared to non-SP cells, which strongly suggested that mouse lens SP cells isolated by FACS are stem cells. | |||||||||||||||
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In analogy to hematopoietic stem cells, solid tumor CSC have been proposed to exhibit high level expression of multidrug transporter family genes, such as ABCG2 and ABCB5, likely resulting in more efficient efflux of chemotherapeutic drugs [13][15]. | |||||||||||||||
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The cellular influx of dasatinib, on the other hand, is not affected by hOCT1 activity, although its efflux may be mediated by ABCB1 and ABCG2.85,86 The intracellular concentration of dasatinib was lower in ABCB1-overexpressing cell lines and was increased in the presence of PSC833, a potent ABCB1 inhibitor.85 The in vitro concentration of dasatinib required to inhibit phosphorylation of CrkL by 50% (dasatinib IC50) was higher in the ABCB1-overexpressing cell lines compared to parental cell lines (100 nM versus 7 nM), and this was reduced to 8 nM with the addition of PSC833.85 Similar results were also seen in the ABCG2-overexpressing cell lines, suggesting that high levels of ABCG2 reduced dasatinib intracellular concentration, leading to an increased dasatinib IC50, which can be modulated with ABCG2 inhibitors.85 | |||||||||||||||
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BCRP protein expression was measured flow cytometrically with the monoclonal antibody (mAb) BXP-21. | |||||||||||||||
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Hence, we examined the effects of indomethacin and dexamethasone on BCRP expression in MCF cells. | |||||||||||||||
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Overexpression of ABC transporters such as Pgp, MRP and BCRP has been shown to be responsible for the major portion of MDR. | |||||||||||||||
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Imatinib has been reported to be a substrate and/or an inhibitor for the ABCG2 drug efflux pump which is overexpressed in many human tumors and also found to be functionally expressed in CML stem cells.64,83,84 The drug transporter hOCT1 mediates the active transport of imatinib into cells, and inhibition of hOCT1 decreases the intracellular concentration of imatinib, which may predict for a less favorable molecular response.65,66 | |||||||||||||||
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Imatinib has been reported to be a substrate and/or an inhibitor for the ABCG2 drug efflux pump which is overexpressed in many human tumors and also found to be functionally expressed in CML stem cells.64,83,84 The drug transporter hOCT1 mediates the active transport of imatinib into cells, and inhibition of hOCT1 decreases the intracellular concentration of imatinib, which may predict for a less favorable molecular response.65,66 | |||||||||||||||
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Dexamethasone downregulates BCRP mRNA and protein expression in breast cancer cell lines. | |||||||||||||||
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It is hypothesized that anti-inflammatory drugs regulate breast cancer resistance protein (BCRP) expression. | |||||||||||||||
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