Nuclear receptor that acts as a transcription factor regulating genes involved in the metabolism and excretion of xenobiotics, drugs, and endogenous compounds. Activated by a broad range of endogenous steroids (e.g. pregnenolone, progesterone) and xenobiotics, including the antibiotic rifampicin and certain plant-derived metabolites. Upon ligand binding, translocates to the nucleus, forms a heterodimer with the retinoid X receptor/RXR, and binds to response elements in target promoters, leading to transcriptional activation.
Target genes include cytochrome P450 enzymes such as CYP3A4 and ATP-binding cassette transporters including ABCB1/MDR1
Heterodimer with RXR. Interacts with NCOA1. Interacts (via domain NR LBD) with CRY1 and CRY2 in a ligand-dependent manner (By similarity).
Interacts with FBXO44; this interaction promotes NR1I2 ubiquitination and proteasomal degradation (PubMed:37969738)
Expressed in liver, colon and small intestine
No mutation information available.
Genes with an experimentally identified or computationally predicted synthetic-lethal relationship to NR1I2, aggregated across our SSL data sources. Click any partner node to view that gene’s page.
Nodes and edges are coloured by the SSL data source. Partners appearing in more than one source are shown in grey.
Total Trials Found: 5
| NCT ID | Condition | Brief Title | Phase | Status |
|---|---|---|---|---|
| NCT00985270 | Glucose Tolerance | Pregnane X Receptor (PXR) Agonist Rifampicin Effects on Glucose, Lipid and Hormone Homeostasis | PHASE4 | COMPLETED |
| NCT01690104 | Blood Pressure Regulation | The Effect of PXR Activation on Blood Pressure Regulation | PHASE4 | COMPLETED |
| NCT00621309 | Adverse Drug Interactions | Sulforaphane as an Antagonist to Human PXR-mediated Drug-drug Interactions | PHASE1 | COMPLETED |
| NCT01293422 | Glucose Metabolism | Effects of Pregnane X Receptor (PXR) Activation on Human Glucose, Lipid and Hormone Homeostasis | PHASE4 | COMPLETED |
| NCT04089501 | Inflammatory Bowel Diseases | The Role of the Pregnane X Receptor (PXR) in Indole Signaling and Intestinal Permeability in Inflammatory Bowel Disease | N/A | COMPLETED |