ArticleBritish journal of pharmacology2008
Comparison of the induction profile for drug disposition proteins by typical nuclear receptor activators in human hepatic and intestinal cells.
Article in British journal of pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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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.
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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
33 citing papers in PubMed, 112 citations in OpenAlex.
- Pharmacometabolomics of trabectedin in metastatic soft tissue sarcoma patients.Frontiers in pharmacology · 2023Article
- Dexamethasone is a dose-dependent perpetrator of drug-drug interactions: implications for use in people living with HIV.The Journal of antimicrobial chemotherapy · 2022Article
- Role of Bile Acids and Nuclear Receptors in Acupuncture in Improving Crohn's Disease.Evidence-based complementary and alternative medicine : eCAM · 2022Review
- Expression dynamics of pregnane X receptor-controlled genes in 3D primary human hepatocyte spheroids.Archives of toxicology · 2022Article
- Effect of Crohn's Disease on Villous Length and CYP3A4 Expression in the Pediatric Small Intestine.Clinical and translational science · 2021Observational
- Cytochrome P450 expression, induction and activity in human induced pluripotent stem cell-derived intestinal organoids and comparison with primary human intestinal epithelial cells and Caco-2 cells.Archives of toxicology · 2021Article
- The constitutive androstane receptor and pregnane X receptor in the brain.British journal of pharmacology · 2020Review
- Regulation of hepatic P-gp expression and activity by genistein in rats.Archives of toxicology · 2020Article
- Clinical relevance of St. John's wort drug interactions revisited.British journal of pharmacology · 2020Review
- Nuclear Receptors Regulate Intestinal Inflammation in the Context of IBD.Frontiers in immunology · 2019Review
- Gancao (Glycyrrhizae Radix) provides the main contribution to Shaoyao-Gancao decoction on enhancements of CYP3A4 and MDR1 expression via pregnane X receptor pathway in vitro.BMC complementary and alternative medicine · 2018Article
- Clinical Investigation of Coproporphyrins as Sensitive Biomarkers to Predict Mild to Strong OATP1B-Mediated Drug-Drug Interactions.Clinical pharmacokinetics · 2018Article
- Differential regulation of intestinal efflux transporters by pregnancy in mice.Xenobiotica; the fate of foreign compounds in biological systems · 2017Article
- Constitutive androstane receptor regulates the intestinal mucosal response to injury.British journal of pharmacology · 2017Article
- Drug-Drug Interactions, Effectiveness, and Safety of Hormonal Contraceptives in Women Living with HIV.Drug safety · 2016Review
- Prediction of Intravenous Busulfan Clearance by Endogenous Plasma Biomarkers Using Global Pharmacometabolomics.Metabolomics : Official journal of the Metabolomic Society · 2016Article
- Characterizing drug-metabolizing enzymes and transporters that areActa pharmaceutica Sinica. B · 2016Article
- Prediction of Drug-Drug Interactions Arising from CYP3A induction Using a Physiologically Based Dynamic Model.Drug metabolism and disposition: the biological fate of chemicals · 2016Article
- A retrospective analysis of patient-specific factors on voriconazole clearance.Journal of pharmaceutical health care and sciences · 2016Article
- Modulation of P-glycoprotein at the Human Blood-Brain Barrier by Quinidine or Rifampin Treatment: A Positron Emission Tomography Imaging Study.Drug metabolism and disposition: the biological fate of chemicals · 2015Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeCertain nuclear receptors (NRs) such as the constitutive androstane receptor (CAR), pregnane X receptor (PXR) and farnesoid X receptor (FXR) mediate induction of some cytochrome P450 enzymes and ABC transporters but conflicting reports exist. The purpose of this study was to assess the reasons for these discrepancies and use a standardized approach to compare activators of NRs. EXPERIMENTAL APPROACH: Dexamethasone, pregnenolone 16alpha-carbonitrile, rifampicin, phenobarbital and chenodeoxycholic acid were incubated with HepG2, Caco-2 and cryopreserved human hepatocytes prior to analysis of mRNA and protein for CYP2B6, CYP3A4, CYP3A5, ABCB1, ABCC1, ABCC2, PXR, CAR and FXR. KEY
resultsDexamethasone significantly up-regulated PXR, CYP3A4 and ABCB1 expression in HepG2 and Caco-2 cells. As a result, including dexamethasone as a media supplement masked the induction of these genes by pregnenolone 16alpha-carbonitrile, which may explain discrepancies between previous reports. In the absence of dexamethasone, significant activator-dependent induction was observed in all cell types. Significant correlations were observed between the fold increase in mRNA and in protein, which were, for most instances, logarithmic. Changes in mRNA expression were greater in cell lines than primary cells but for most transcripts correlations were observed between fold increases in HepG2 and hepatocytes. CONCLUSIONS AND IMPLICATIONS: Clearly, no in vitro system can imitate the physiology of a hepatocyte or intestinal cell within an intact organ in vivo, but these data explain some of the discrepancies reported between laboratories and have important implications for study design.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.