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| Description
| - Recent findings show that colchicine (COL) in submicromolar concentrations downregulates the expression of major drug-metabolizing P450 enzymes in human hepatocytes. Concomitantly, the expression of pregnane X receptor (PXR) and constitutive androstane receptor (CAR) was diminished by COL, whereas expression of glucocorticoid receptor (GR) remained unaltered. A tentative mechanism is perturbation of the GR-PXR/CAR-CYP2/3 signaling cascade, resulting in restricted transcriptional activity of GR receptor by colchicine. In this work we focused on 10-demethylcolchicine (colchiceine; EIN), a structural analogue and a putative metabolite of COL that lacks tubulin-binding activity. We investigated the effects of EIN on the expression of PXR, CAR, and GR receptors in primary cultures of human hepatocytes. In contrast with the effects of COL, EIN does not alter the expression of PXR, CAR, and/or GR receptors mRNAs. In addition, EIN had no effects on transcriptional activities of PXR, CAR, and GR receptors in r
- Recent findings show that colchicine (COL) in submicromolar concentrations downregulates the expression of major drug-metabolizing P450 enzymes in human hepatocytes. Concomitantly, the expression of pregnane X receptor (PXR) and constitutive androstane receptor (CAR) was diminished by COL, whereas expression of glucocorticoid receptor (GR) remained unaltered. A tentative mechanism is perturbation of the GR-PXR/CAR-CYP2/3 signaling cascade, resulting in restricted transcriptional activity of GR receptor by colchicine. In this work we focused on 10-demethylcolchicine (colchiceine; EIN), a structural analogue and a putative metabolite of COL that lacks tubulin-binding activity. We investigated the effects of EIN on the expression of PXR, CAR, and GR receptors in primary cultures of human hepatocytes. In contrast with the effects of COL, EIN does not alter the expression of PXR, CAR, and/or GR receptors mRNAs. In addition, EIN had no effects on transcriptional activities of PXR, CAR, and GR receptors in r (en)
- Nová data ukazují, že kolchicin (COL) přítomný submikromolárních koncentracích snižuje expresi důležitých enzymů rodiny P450 v lidských hepatocytech. Exprese pregnanového X receptoru (PXR) a konstitutivního androstanového receptoru (CAR) byla snížena vlivem COL, naproti tomu exprese glukokortikoidního receptoru (GR) ovlivněna nebyla. Předpokládaným mechanismem je porušení signální kaskády GR-PXR/CAR-CYP2/3, což má za následek omezenou transkripční aktivitu GR. V této práci jsme se soustředili na 10-demethylkolchicein (EIN), strukturní analog a předpokládaný metabolit COL, ovšem postrádající schopnost vázat se na tubulin. Na rozdíl od COL, EIN neměnil expresi mRNA PXR, CAR, a/nebo GR receptorů. Navíc, EIN neměl žádný vliv na transkripční aktivitu PXR, CAR a GR receptorů, která byla hodnocena s pomocí reportérových esejí. Vzhledem k tomu, že COL a EIN jsou si strukturně velmi blízcí a liší se pouze schopností vázat se na tubulin, naše výsledky naznačují, že ovlivnění signální kaskády GR-PXR/CAR-CYP2/3 j (cs)
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| Title
| - Expression and transcriptional activities of nuclear receptors involved in regulation of drug-metabolizing enzymes are not altered by colchicine: focus on PXR, CAR, and GR in primary human hepatocytes
- Expression and transcriptional activities of nuclear receptors involved in regulation of drug-metabolizing enzymes are not altered by colchicine: focus on PXR, CAR, and GR in primary human hepatocytes (en)
- Exprese a transkripční aktivity jaderných receptorů zapojených do regulace enzymů metabolizujících léčiva nejsou změněny kolchicinem: Zaostřeno na PXR, CAR a GR v primárních lidských hepatocytech (cs)
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| skos:prefLabel
| - Expression and transcriptional activities of nuclear receptors involved in regulation of drug-metabolizing enzymes are not altered by colchicine: focus on PXR, CAR, and GR in primary human hepatocytes
- Expression and transcriptional activities of nuclear receptors involved in regulation of drug-metabolizing enzymes are not altered by colchicine: focus on PXR, CAR, and GR in primary human hepatocytes (en)
- Exprese a transkripční aktivity jaderných receptorů zapojených do regulace enzymů metabolizujících léčiva nejsou změněny kolchicinem: Zaostřeno na PXR, CAR a GR v primárních lidských hepatocytech (cs)
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| skos:notation
| - RIV/61989592:15110/07:00004397!RIV08-MSM-15110___
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| http://linked.open.../vavai/riv/strany
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
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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/61989592:15110/07:00004397
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - human hepatocytes; colchiceine; orphan receptors; drug metabolism (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
| - Cell Biology and Toxicology
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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...UplatneniVysledku
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| http://linked.open...v/svazekPeriodika
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| http://linked.open...iv/tvurceVysledku
| - Dvořák, Zdeněk
- Ulrichová, Jitka
- Modrianský, Martin
- Maurel, Patrick
- Vilarem, M.-J.
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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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