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

Hakkola, J; Bernasconi, C; Coecke, S; Richert, L; Andersson, TB; Pelkonen, O

HERO ID

4933751

Reference Type

Journal Article

Subtype

Review

Year

2018

Language

English

PMID

29527807

HERO ID 4933751
Material Type Review
In Press No
Year 2018
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, J; Bernasconi, C; Coecke, S; Richert, L; Andersson, TB; Pelkonen, O
Journal Basic & Clinical Pharmacology & Toxicology
Volume 123
Issue Suppl 5 Special Issue
Page Numbers 42-50
Abstract Pregnane X receptor (PXR), constitutive androstane receptor (CAR), aryl hydrocarbon receptor (AHR) and peroxisome proliferator-activated receptor (PPAR) 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.
Doi 10.1111/bcpt.13004
Pmid 29527807
Wosid WOS:000445849900006
Is Certified Translation No
Dupe Override No
Conference Location Helsinki, Finland
Conference Name Joint European-Consensus-Platform-for-Alternatives (ECOPA) and Scandinavian-Society-for-Cell-Toxicology (SSCT) Workshop on Up-to-Date in Vitro Approaches in Regulatory Risk Assessment and Disease Modeling
Conference Date June 14-16, 2017
Is Public Yes
Language Text English
Is Peer Review Yes
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