ArticlePharmaceutical research2006
Metabolic and efflux properties of Caco-2 cells stably transfected with nuclear receptors.
Article in Pharmaceutical research, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
4 citing papers in PubMed, 29 citations in OpenAlex.
- Reliability of in vitro data for the mechanistic prediction of brain extracellular fluid pharmacokinetics of P-glycoprotein substrates in vivo; are we scaling correctly?Journal of pharmacokinetics and pharmacodynamics · 2025Article
- Analyzing the metabolic fate of oral administration drugs: A review and state-of-the-art roadmap.Frontiers in pharmacology · 2022Review
- Development of Caco-2 cells expressing four CYPs via a mammalian artificial chromosome.BMC biotechnology · 2020Article
- Up-regulating CYP3A4 expression in C3A cells by transfection with a novel chimeric regulator of hPXR-p53-AD.PloS one · 2014Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo characterise in detail the patterns of expression and functional activities of CYP and efflux pump genes in Caco-2 cells stably transfected with human Pregnane X Receptor or murine Constitutive Androstane Receptor. MATERIALS AND
methodsCell lines transfected with nuclear receptors were treated with established ligands, and gene expression of CYP and efflux pump genes were quantified by qRT-PCR and Western blot. P-glycoprotein activity was assessed by measuring calcein-AM accumulation and bidirectional permeability coefficients of digoxin and quinidine. CYP activities were measured with both fluorescent and non-fluorescent substrates.
resultshPXR and mCAR upregulated some CYP and efflux pump genes ligand dependently. P-glycoprotein level was increased, but CYP3A4 protein remained below the limit of detection. P-glycoprotein activity was markedly elevated in Caco/mCAR cells and more modestly in Caco/hPXR cells. CYP3A4 activity remained lower than that in vitamin D-treated Caco-2 cells.
conclusionsNuclear receptors can modulate the expression of metabolic genes in Caco-2 cells, but the overall level of metabolism could not be efficiently controlled. P-glycoprotein activity increased, but CYP activities remained very low.
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Registered trials
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