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Regulation of CAR and PXR Expression in Health and Disease

Pregnane X receptor (PXR, NR1I2) and constitutive androstane receptor (CAR, NR1I3) are members of the nuclear receptor superfamily that mainly act as ligand-activated transcription factors. Their functions have long been associated with the regulation of drug metabolism and disposition, and it is no...

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Autores principales: Daujat-Chavanieu, Martine, Gerbal-Chaloin, Sabine
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7692647/
https://www.ncbi.nlm.nih.gov/pubmed/33142929
http://dx.doi.org/10.3390/cells9112395
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author Daujat-Chavanieu, Martine
Gerbal-Chaloin, Sabine
author_facet Daujat-Chavanieu, Martine
Gerbal-Chaloin, Sabine
author_sort Daujat-Chavanieu, Martine
collection PubMed
description Pregnane X receptor (PXR, NR1I2) and constitutive androstane receptor (CAR, NR1I3) are members of the nuclear receptor superfamily that mainly act as ligand-activated transcription factors. Their functions have long been associated with the regulation of drug metabolism and disposition, and it is now well established that they are implicated in physiological and pathological conditions. Considerable efforts have been made to understand the regulation of their activity by their cognate ligand; however, additional regulatory mechanisms, among which the regulation of their expression, modulate their pleiotropic effects. This review summarizes the current knowledge on CAR and PXR expression during development and adult life; tissue distribution; spatial, temporal, and metabolic regulations; as well as in pathological situations, including chronic diseases and cancers. The expression of CAR and PXR is modulated by complex regulatory mechanisms that involve the interplay of transcription factors and also post-transcriptional and epigenetic modifications. Moreover, many environmental stimuli affect CAR and PXR expression through mechanisms that have not been elucidated.
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spelling pubmed-76926472020-11-28 Regulation of CAR and PXR Expression in Health and Disease Daujat-Chavanieu, Martine Gerbal-Chaloin, Sabine Cells Review Pregnane X receptor (PXR, NR1I2) and constitutive androstane receptor (CAR, NR1I3) are members of the nuclear receptor superfamily that mainly act as ligand-activated transcription factors. Their functions have long been associated with the regulation of drug metabolism and disposition, and it is now well established that they are implicated in physiological and pathological conditions. Considerable efforts have been made to understand the regulation of their activity by their cognate ligand; however, additional regulatory mechanisms, among which the regulation of their expression, modulate their pleiotropic effects. This review summarizes the current knowledge on CAR and PXR expression during development and adult life; tissue distribution; spatial, temporal, and metabolic regulations; as well as in pathological situations, including chronic diseases and cancers. The expression of CAR and PXR is modulated by complex regulatory mechanisms that involve the interplay of transcription factors and also post-transcriptional and epigenetic modifications. Moreover, many environmental stimuli affect CAR and PXR expression through mechanisms that have not been elucidated. MDPI 2020-10-31 /pmc/articles/PMC7692647/ /pubmed/33142929 http://dx.doi.org/10.3390/cells9112395 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Daujat-Chavanieu, Martine
Gerbal-Chaloin, Sabine
Regulation of CAR and PXR Expression in Health and Disease
title Regulation of CAR and PXR Expression in Health and Disease
title_full Regulation of CAR and PXR Expression in Health and Disease
title_fullStr Regulation of CAR and PXR Expression in Health and Disease
title_full_unstemmed Regulation of CAR and PXR Expression in Health and Disease
title_short Regulation of CAR and PXR Expression in Health and Disease
title_sort regulation of car and pxr expression in health and disease
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7692647/
https://www.ncbi.nlm.nih.gov/pubmed/33142929
http://dx.doi.org/10.3390/cells9112395
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