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Article
Open AccessA novel differentiated HuH-7 cell model to examine bile acid metabolism, transport and cholestatic hepatotoxicity
Hepatic cell lines serve as economical and reproducible alternatives for primary human hepatocytes. However, the utility of hepatic cell lines to examine bile acid homeostasis and cholestatic toxicity is limit...
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Article
Open AccessDeficient neurotransmitter systems and synaptic function in frontotemporal lobar degeneration—Insights into disease mechanisms and current therapeutic approaches
Frontotemporal lobar degeneration (FTLD) comprises a heterogenous group of fatal neurodegenerative diseases and, to date, no validated diagnostic or prognostic biomarkers or effective disease-modifying therapi...
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Article
Open AccessFunctional impact of cytochrome P450 3A (CYP3A) missense variants in cattle
Cytochrome P450 3A is the most important CYP subfamily in humans, and CYP3A4/CYP3A5 genetic variants contribute to inter-individual variability in drug metabolism. However, no information is available for bovi...
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Protocol
A Reverse Transfection Method for Screening of Nuclear Receptor Activators
Reporter assays are useful to study nuclear receptor activation and for example to evaluate the propensity of novel drug candidates to cause induction of drug-metabolizing cytochrome P450 enzymes. Here, we des...
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Article
Open AccessDHCR24 exerts neuroprotection upon inflammation-induced neuronal death
DHCR24, involved in the de novo synthesis of cholesterol and protection of neuronal cells against different stress conditions, has been shown to be selectively downregulated in neurons of the affected brain ar...
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Article
A liquid chromatography-tandem mass spectrometry analysis of nine cytochrome P450 probe drugs and their corresponding metabolites in human serum and urine
Cocktail phenoty** using specific probe drugs for cytochrome P450 (CYP) enzymes provides information on the real-time activity of multiple CYPs. We investigated different sample preparation techniques and va...
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Article
Open AccessFisetin and luteolin protect human retinal pigment epithelial cells from oxidative stress-induced cell death and regulate inflammation
Degeneration of retinal pigment epithelial (RPE) cells is a clinical hallmark of age-related macular degeneration (AMD), the leading cause of blindness among aged people in the Western world. Both inflammation...
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Article
Regulation of gene expression by CAR: an update
The constitutive androstane receptor (CAR), a member of the nuclear receptor superfamily, is a well-known xenosensor that regulates hepatic drug metabolism and detoxification. CAR activation can be elicited by...
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Article
Inhibition and induction of human cytochrome P450 enzymes: current status
Variability of drug metabolism, especially that of the most important phase I enzymes or cytochrome P450 (CYP) enzymes, is an important complicating factor in many areas of pharmacology and toxicology, in drug...
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Article
Metabolic and Efflux Properties of Caco-2 Cells Stably Transfected with Nuclear Receptors
To 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 R...
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Article
Molecular dynamics simulations of the human CAR ligand-binding domain: deciphering the molecular basis for constitutive activity
The constitutive androstane receptor (CAR) belongs to the superfamily of nuclear-hormone receptors that function as ligand-activated transcription factors. CAR plays an essential role in the metabolism of xeno...
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Article
A Novel Drug-Regulated Gene Expression System Based on the Nuclear Receptor Constitutive Androstane Receptor (CAR)
Purpose. To develop and characterize a new drug-regulated gene expression system based on the nuclear receptor constitutive androstane receptor (CAR).
