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| Description
| - V prezentované studii jsme studavali hypotézu, zda kyselina valproová v terapeuticky relevantních koncentracích může ovlivnit expresi CYP3A4 a MDR1 aktivací konstitutivního androstanového receptoru (CAR) nebo pregnanového X receptoru (PXR). Interakce kyseliny valproové s CAR a PXR byla studována pomocí luciferázových reporterových experimentů, RT-PCR v reálném čase, %22electrophoretic mobility shift assay%22 (EMSA) a nakonec jsme analyzovali změnu biotransformační aktivity CYP3A4. Luciferázové reporterové studie v HepG2 buněčné linii prokázaly, že kyselina valproová aktivuje promotor CYP3A4 skrze CAR a PXR. Naproti tomu, v případě MDR1 byla změna transkripční aktivity pozorována pouze v momentě, kdy HepG2 buňky exprimovaly exogenní PXR. Tato data korelovala s výsledky, které jsme získali real time RT-PCR analýzou exprese CYP3A4 a MDR mRNA v LS174T buňkách transientně transfekovaných expresním vektorem pro CAR nebo PXR. Zvýšená exprese CYP3A4 mRNA byla pozorována taktéž při analýze lidských primá (cs)
- In our study, we tested the hypothesis whether valproic acid (VPA) in therapeutic concentrations has potential to affect expression of CYP3A4 and MDR1 via constitutive androstane receptor (CAR) and pregnane X receptor (PXR) pathways. Interaction of VPA with CAR and PXR nuclear receptors was studied using luciferase reporter assays, real-time reverse transcriptase polymerase chain reaction (RT-PCR), electrophoretic mobility shift assay (EMSA), and analysis of CYP3A4 catalytic activity. Using transient transfection reporter assays in HepG2 cells, VPA was recognized to activate CYP3A4 promoter via CAR and PXR pathways. By contrast, a significant effect of VPA on MDR1 promoter activation was observed only in CAR-cotransfected HepG2 cells. These data well correlated with up-regulation of CYP3A4 and MDR1 mRNAs analyzed by real-time RT-PCR in cells transfected with expression vectors encoding CAR or PXR and treated with VPA. In addition, VPA significantly up-regulated CYP3A4 mRNA in primary hepatocytes and a
- In our study, we tested the hypothesis whether valproic acid (VPA) in therapeutic concentrations has potential to affect expression of CYP3A4 and MDR1 via constitutive androstane receptor (CAR) and pregnane X receptor (PXR) pathways. Interaction of VPA with CAR and PXR nuclear receptors was studied using luciferase reporter assays, real-time reverse transcriptase polymerase chain reaction (RT-PCR), electrophoretic mobility shift assay (EMSA), and analysis of CYP3A4 catalytic activity. Using transient transfection reporter assays in HepG2 cells, VPA was recognized to activate CYP3A4 promoter via CAR and PXR pathways. By contrast, a significant effect of VPA on MDR1 promoter activation was observed only in CAR-cotransfected HepG2 cells. These data well correlated with up-regulation of CYP3A4 and MDR1 mRNAs analyzed by real-time RT-PCR in cells transfected with expression vectors encoding CAR or PXR and treated with VPA. In addition, VPA significantly up-regulated CYP3A4 mRNA in primary hepatocytes and a (en)
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| Title
| - Valproic acid induces CYP3A4 and MDR1 gene expression by activation of constitutive androstane receptor and pregnane X receptor pathways
- Kyselina valproová indukuje CYP3A4 a MDR1 genovou expresiaktivací konstitutivního androstanového receptoru a preganového X receptoru (cs)
- Valproic acid induces CYP3A4 and MDR1 gene expression by activation of constitutive androstane receptor and pregnane X receptor pathways (en)
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| skos:prefLabel
| - Valproic acid induces CYP3A4 and MDR1 gene expression by activation of constitutive androstane receptor and pregnane X receptor pathways
- Kyselina valproová indukuje CYP3A4 a MDR1 genovou expresiaktivací konstitutivního androstanového receptoru a preganového X receptoru (cs)
- Valproic acid induces CYP3A4 and MDR1 gene expression by activation of constitutive androstane receptor and pregnane X receptor pathways (en)
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| skos:notation
| - RIV/60162694:G44__/07:00001732!RIV09-MO0-G44_____
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
| - P(GA303/07/0128), V, Z(MO0FVZ0000501), Z(MSM6198959216)
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| http://linked.open...iv/cisloPeriodika
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| http://linked.open...vai/riv/dodaniDat
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| http://linked.open...aciTvurceVysledku
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| http://linked.open.../riv/druhVysledku
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| http://linked.open...iv/duvernostUdaju
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| http://linked.open...titaPredkladatele
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| http://linked.open...dnocenehoVysledku
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| http://linked.open...ai/riv/idVysledku
| - RIV/60162694:G44__/07:00001732
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - valproic acid; constitutive androstane receptor; pregnane X receptor; gene reporter assay; transcriptional activation; up-regulation; CYP3A4; MDR1; P-glycoprotein, HepG2, primary human hepatocytes (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
| - US - Spojené státy americké
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
| - Drug Metabolism and Disposition
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| http://linked.open...in/vavai/riv/obor
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| http://linked.open...ichTvurcuVysledku
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| http://linked.open...cetTvurcuVysledku
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| http://linked.open...vavai/riv/projekt
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| http://linked.open...UplatneniVysledku
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| http://linked.open...v/svazekPeriodika
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| http://linked.open...iv/tvurceVysledku
| - Dvořák, Zdeněk
- Pávek, Petr
- Ulrichová, Jitka
- Vrzal, Radim
- Červený, Lukáš
- Anzenbacher, Pavel
- Anzenbacherová, Eva
- Štaud, František
- Švecová, Lucie
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| http://linked.open...n/vavai/riv/zamer
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| issn
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| number of pages
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| http://localhost/t...ganizacniJednotka
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