The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.
- J. Lehmann, D. D. Mckee, M. Watson, T. Willson, J. Moore, S. Kliewer
- BiologyJournal of Clinical Investigation
- 1 September 1998
The identification of a human (h) orphan nuclear receptor, termed the pregnane X receptor (PXR), that binds to a response element in the CYP3A4 promoter and is activated by a range of drugs known to induce CYP 3A4 expression is reported.
A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis.
- B. Goodwin, S. A. Jones, S. Kliewer
- Biology, ChemistryMolecules and Cells
- 1 September 2000
Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis.
- T. Inagaki, Mihwa Choi, S. Kliewer
- Biology, ChemistryCell Metabolism
- 1 October 2005
An Orphan Nuclear Receptor Activated by Pregnanes Defines a Novel Steroid Signaling Pathway
- S. Kliewer, John T. Moore, J. Lehmann
- Biology, ChemistryCell
- 9 January 1998
The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity
- J. Staudinger, B. Goodwin, S. Kliewer
- BiologyProceedings of the National Academy of Sciences…
- 13 March 2001
It is proposed that PXR serves as a physiological sensor of LCA, and coordinately regulates gene expression to reduce the concentrations of this toxic bile acid, and suggest that PxR agonists may prove useful in the treatment of human cholestatic liver disease.
Bile acids: natural ligands for an orphan nuclear receptor.
- D. Parks, S. Blanchard, J. Lehmann
- Biology, ChemistryScience
- 21 May 1999
Results provide evidence for a nuclear bile acid signaling pathway that may regulate cholesterol homeostasis and modulated interaction of FXR with a peptide derived from steroid receptor coactivator 1.
Endocrine regulation of the fasting response by PPARalpha-mediated induction of fibroblast growth factor 21.
- T. Inagaki, Paul A. Dutchak, S. Kliewer
- Biology, MedicineCell Metabolism
- 6 June 2007
Orphan Nuclear Receptors Constitutive Androstane Receptor and Pregnane X Receptor Share Xenobiotic and Steroid Ligands*
- L. Moore, D. Parks, S. Kliewer
- Biology, ChemistryJournal of Biological Chemistry
- 19 May 2000
It is demonstrated that several of the compounds that regulate mouse and human CAR, including natural steroids, bind directly to the receptors and suggest that CAR, like PXR, is a steroid receptor that is capable of recognizing structurally diverse compounds.
Regulation of Multidrug Resistance-associated Protein 2 (ABCC2) by the Nuclear Receptors Pregnane X Receptor, Farnesoid X-activated Receptor, and Constitutive Androstane Receptor*
- H. R. Kast, B. Goodwin, P. Edwards
- Biology, ChemistryJournal of Biological Chemistry
- 25 January 2002
It is demonstrated that MRP2 is regulated by three distinct nuclear receptor signaling pathways that converge on a common response element in the 5′-flanking region of this gene.
An Antidiabetic Thiazolidinedione Is a High Affinity Ligand for Peroxisome Proliferator-activated Receptor Îł (PPARÎł) (*)
- J. Lehmann, L. Moore, T. Smith-Oliver, W. Wilkison, T. Willson, S. Kliewer
- Biology, ChemistryJournal of Biological Chemistry
- 2 June 1995
It is reported that thiazolidinediones are potent and selective activators of peroxisome proliferator-activated receptor Îł (PPARÎł), a member of the nuclear receptor superfamily recently shown to function in adipogenesis, and raised the intriguing possibility that PPARÎł is a target for the therapeutic actions of this class of compounds.
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