Title: Cytochrome P450 Induction and Xeno-Sensing Receptors Pregnane X Receptor, Constitutive Androstane Receptor, Aryl Hydrocarbon Receptor and Peroxisome Proliferator-Activated Receptor α at the Crossroads of Toxicokinetics and Toxicodynamics
Authors: HAKKOLA JUKKABERNASCONI CAMILLACOECKE SANDRARICHERT LYSIANEANDERSSON TOMMY BPELKONEN OLAVI
Citation: BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY vol. 123 no. S5
Publisher: WILEY-BLACKWELL
Publication Year: 2018
JRC N°: JRC110859
ISSN: 1742-7835 (online)
URI: http://publications.jrc.ec.europa.eu/repository/handle/JRC110859
DOI: 10.1111/bcpt.13004
Type: Articles in periodicals and books
Abstract: Pregnane X receptor (PXR), constitutive androstane receptor (CAR), aryl hydrocarbon receptor (AHR) and peroxisome proliferator‐activated receptor α (PPARα) are ligand‐activated transcription factors that regulate expression of many xenobiotic‐metabolizing enzymes including several cytochrome P450 (CYP) enzymes. Many xenobiotics induce CYP enzymes through these intracellular receptors and consequently affect toxicokinetics and possible metabolic activation of the receptor ligands and other xenobiotics utilizing similar metabolic pathways. However, it is now apparent that the xenobiotic receptors regulate also many endogenous functions and signalling pathways, and xenobiotic exposure thus may dysregulate an array of fundamental cell functions. This MiniReview surveys and discusses the multifaceted roles of xenobiotic receptors, for which CYP induction may serve as the first alert and possibly a biomarker for exposure to xenobiotics. With the current emergence of the adverse outcome pathway (AOP) concept, these receptors are being and will be assigned as molecular initiating events or key events in numerous discrete toxicity pathways.
JRC Directorate:Health, Consumers and Reference Materials

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