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Target intelligence / Profile preview
Pregnane X Receptor (PXR)
- Target
- PXR
- Molecular classification
- Nuclear Receptor, Transcription Factor
01
Overview
The pregnane X receptor (PXR) is a nuclear receptor that functions as a ligand-activated transcription factor. It plays a crucial role in sensing and detoxifying foreign substances (xenobiotics) and endogenous compounds, primarily in the liver and intestine. Upon activation, PXR upregulates genes involved in drug metabolism and transport, influencing drug pharmacokinetics, drug-drug interactions, and the risk of metabolic diseases.
- Other names
- Steroid and Xenobiotic ReceptorSXRBXRNuclear Receptor Subfamily 1, Group I, Member 2NR1I2Orphan Nuclear Receptor PAR1/ONR1/PAR2
02
Mechanism of action
Ligand binding induces translocation to the nucleus, heterodimerization with RXR, and binding to response elements on target genes, leading to altered gene transcription.
03
Biological functions
Xenobiotic sensingEndobiotic sensingDetoxificationRegulation of gene transcriptionDrug metabolism regulationGlucose homeostasisLipid homeostasisBile acid homeostasis
04
Disease associations
Metabolic diseasesDiabetesObesityDrug resistanceInflammatory bowel diseaseHepatic steatosisDrug-induced toxicityCarcinogenesis
05
Safety considerations
Drug-drug interactions due to altered drug metabolismChemotherapeutic resistance via MDR1 upregulation
06
Interacting drugs
Rifampicin
7 more in the full profile.
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