Nuclear receptor PXR, transcriptional circuits and metabolic relevance
- PMID: 21295138
- PMCID: PMC3111845
- DOI: 10.1016/j.bbadis.2011.01.014
Nuclear receptor PXR, transcriptional circuits and metabolic relevance
Abstract
The pregnane X receptor (PXR, NR1I2) is a ligand activated transcription factor that belongs to the nuclear hormone receptor (NR) superfamily. PXR is highly expressed in the liver and intestine, but low levels of expression have also been found in many other tissues. PXR plays an integral role in xenobiotic and endobiotic metabolism by regulating the expression of drug-metabolizing enzymes and transporters, as well as genes implicated in the metabolism of endobiotics. PXR exerts its transcriptional regulation by binding to its DNA response elements as a heterodimer with the retinoid X receptor (RXR) and recruitment of a host of coactivators. The biological and physiological implications of PXR activation are broad, ranging from drug metabolism and drug-drug interactions to the homeostasis of numerous endobiotics, such as glucose, lipids, steroids, bile acids, bilirubin, retinoic acid, and bone minerals. The purpose of this article is to provide an overview on the transcriptional circuits and metabolic relevance controlled by PXR. This article is part of a Special Issue entitled: Translating Nuclear Receptors from Health to Disease.
Copyright © 2010 Elsevier B.V. All rights reserved.
Figures
References
-
- Kliewer SA, et al. An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway. Cell. 1998;92(1):73–82. - PubMed
-
- Francis GA, et al. Nuclear receptors and the control of metabolism. Annu Rev Physiol. 2003;65:261–311. - PubMed
-
- Jones SA, et al. The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution. Mol Endocrinol. 2000;14(1):27–39. - PubMed
-
- Chirulli V, et al. CAR and PXR expression and inducibility of CYP2B and CYP3A activities in rat and rabbit lungs. Life Sci. 2005;76(22):2535–46. - PubMed
Publication types
MeSH terms
Substances
Grants and funding
LinkOut - more resources
Full Text Sources
Molecular Biology Databases
