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Target intelligence / Profile preview
Nuclear receptor subfamily 1 group I member 2 (NR1I2)
- Target
- NR1I2
- Molecular classification
- Nuclear receptor, Transcription factor
01
Overview
Nuclear receptor subfamily 1 group I member 2 (NR1I2), also known as the Pregnane X Receptor (PXR), is a ligand-activated transcription factor that acts as a sensor for endogenous steroids and exogenous substances. Upon ligand binding, it heterodimerizes with RXRα and upregulates genes involved in detoxification pathways, influencing drug metabolism and transport. It is highly expressed in liver and intestines and plays a role in pharmacokinetics and drug-drug interactions.
- Other names
- Pregnane X ReceptorPXRSXRPARQPARBXRONR1
02
Mechanism of action
Ligand-dependent activation of transcription via heterodimerization with RXRα and binding to response elements on target gene promoters, leading to upregulation of genes involved in detoxification pathways (e.g., CYP3A4, ABCB1/MDR1).
03
Biological functions
Xenobiotic catabolic processSteroid metabolic processRegulation of gene expressionDetoxificationClearance of foreign substances
04
Disease associations
Drug-drug interactionsAltered steroid metabolismChronic exposure to environmental chemicals
05
Safety considerations
Drug-drug interactions due to competition for activation/inhibitionPotential for altered drug metabolism and efficacy/toxicity profiles
06
Interacting drugs
Rifampicin
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