Pregnane-X Receptor (PXR) agonists

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What is the most important effect of Pregnane-X Receptor (PXR) agonists?

The single most important effect of Pregnane-X Receptor (PXR) agonists activation is transcriptional induction of CYP3A4 and related drug-metabolizing enzymes and transporters - PXR is considered the master xenobiotic receptor governing this system (2)

What is the mode of action for the interaction of Pregnane-X Receptor (PXR) agonists with the Pregnane-X Receptor (PXR)?

Once a ligand binds Pregnane-X Receptor (PXR), it heterodimerizes with RXR and upregulates (2, 3, 4):

Phase I enzymes - chiefly CYP3A4 (metabolizes >50% of clinically used drugs), plus […

References (Sources)

CAR and PXR agonists stimulate hepatic bile acid and bilirubin detoxiﬁcation and elimination pathways in mice
Wagner et al. 2005a Hepatology 42: 420-430
PXR: More Than Just a Master Xenobiotic Receptor
Oladimeji & Chen 2018 Mol Pharmacol 93(2): 119-127
Review
Regulation of PXR in drug metabolism: chemical and structural perspectives
Gee et al. 2024 Expert Opin Drug Metab Toxicol 20(1-2): 9-23
Review
The Nuclear Xenobiotic Receptor Pregnane X Receptor: Recent Insights and New Challenges
Orans et al. 2005 Molecular Endocrinology 19(12): 2891-2900
Review

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