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| Description
| - SP600125, specifický inhibitor c-Jun-N-Terminální kinasy (JNK), byl popsán jako ligand a antagonista aryl uhlovodíkového receptoru (AhR) (Joiakim et al. 2003 Drug Metab Dispos 31:1279-82). Zde ukazujeme, že SP600125 není antagonista ale parciální agonista lidského AhR. SP600125 signifikantně indukoval CYP1A1 a CYP1A2 mRNA v primárních lidských hepatocytech a CYP1A1 mRNA v lidských hepatomových buňkách HepG2. Tento účinek byl vyrušen resveratrolem, antagonistou AhR. Konzistentně s recentním pozorováním, SP600125 koncentračně-závisle inhiboval indukci CYP1A1 a CYP1A2 genů prototypickým AhR ligandem 2,3,7,8-tetrachlorodibenzo-p-dioxinem (TCDD) v lidských hepatocytech. Navíc SP600125 vykázal typické chování parciálního agonisty v HepG2 buňkách transientně transfekovaných s reportérovým plasmidem obsahujícím dva invertované opakovanání dioxin responsivního elementu nebo s plasmidem obsahujícím 5´-flanking region lidského CYP1A1 gene. SP600125 transaktivoval reportérové plasmidy s EC50 0.005 uM a 1.89 uM. N (cs)
- SP600125, a specific inhibitor of c-Jun-N-Terminal kinase (JNK), was reported as a ligand and antagonist of aryl hydrocarbon receptor (AhR) [Joiakim A, Mathieu PA, Palermo C, Gasiewicz TA, Reiners Jr JJ. The Jun N terminal kinase inhibitor SP600125 is a ligand and antagonist of the aryl hydrocarbon receptor. Drug Metab Dispos 2003;31(11):1279-82]. Here we show that SP600125 is not an antagonist but a partial agonist of human AhR. SP600125 significantly induced CYP1A1 and CYP1A2 mRNAs in primary human hepatocytes and CYP1A1 mRNA in human hepatoma cells HepG2. This effect was abolished by resveratrol, an antagonist of AhR. Consistent with the recent report, SP600125 dose-dependently inhibited CYP1A1 and CYPIA2 genes induction by a prototype AhR ligand 2,3,7,8-tetrachlorodibenzo-p -dioxin (TCDD) in human hepatocytes. Moreover, SP600125 displayed typical behavior of a partial agonist in HepG2 cells transiently transfected with a reporter plasmid containing two inverted repeats of the dioxin responsive el
- SP600125, a specific inhibitor of c-Jun-N-Terminal kinase (JNK), was reported as a ligand and antagonist of aryl hydrocarbon receptor (AhR) [Joiakim A, Mathieu PA, Palermo C, Gasiewicz TA, Reiners Jr JJ. The Jun N terminal kinase inhibitor SP600125 is a ligand and antagonist of the aryl hydrocarbon receptor. Drug Metab Dispos 2003;31(11):1279-82]. Here we show that SP600125 is not an antagonist but a partial agonist of human AhR. SP600125 significantly induced CYP1A1 and CYP1A2 mRNAs in primary human hepatocytes and CYP1A1 mRNA in human hepatoma cells HepG2. This effect was abolished by resveratrol, an antagonist of AhR. Consistent with the recent report, SP600125 dose-dependently inhibited CYP1A1 and CYPIA2 genes induction by a prototype AhR ligand 2,3,7,8-tetrachlorodibenzo-p -dioxin (TCDD) in human hepatocytes. Moreover, SP600125 displayed typical behavior of a partial agonist in HepG2 cells transiently transfected with a reporter plasmid containing two inverted repeats of the dioxin responsive el (en)
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| Title
| - JNK inhibitor SP600125 is a partial agonist of human aryl hydrocarbon receptor and induces CYP1A1 and CYP1A2 genes in primary human hepatocytes
- SP600125 je parciální atomista lidského aryl uhlovodíkového receptoru a indukuje CYP1A1 a CYP1A2 geny v primárních lidských hepatocytech. (cs)
- JNK inhibitor SP600125 is a partial agonist of human aryl hydrocarbon receptor and induces CYP1A1 and CYP1A2 genes in primary human hepatocytes (en)
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| skos:prefLabel
| - JNK inhibitor SP600125 is a partial agonist of human aryl hydrocarbon receptor and induces CYP1A1 and CYP1A2 genes in primary human hepatocytes
- SP600125 je parciální atomista lidského aryl uhlovodíkového receptoru a indukuje CYP1A1 a CYP1A2 geny v primárních lidských hepatocytech. (cs)
- JNK inhibitor SP600125 is a partial agonist of human aryl hydrocarbon receptor and induces CYP1A1 and CYP1A2 genes in primary human hepatocytes (en)
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| skos:notation
| - RIV/61989592:15310/08:00005344!RIV09-MSM-15310___
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
| - P(GA303/07/0128), S, 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/61989592:15310/08:00005344
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - aryl hydrocarbon receptor; human hepatocytes; c-Jun-N-terminal kinase; SP600125 (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
| - GB - Spojené království Velké Británie a Severního Irska
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
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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
| - Bednář, Petr
- Dvořák, Zdeněk
- Ehrmann, Jiří
- Lemr, Karel
- Pávek, Petr
- Ulrichová, Jitka
- Vrzal, Radim
- Anzenbacherová, Eva
- Jančová, Petra
- Havlík, Roman
- Švecová, Lucie
- Henklová, Pavla
- Maurel, Patrick
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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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| is http://linked.open...avai/riv/vysledek
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