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Ligand

PXR is activated by a large number of endogenous and exogenous chemicals including steroids, antibiotics, antimycotics, bile acids, hyperforin, a constituent of the herbal antidepressant St. John's Wort, and many other herbal compounds.

PXR is activated by a range of compounds that induce CYP3A4, including dexamethasone and rifampicin.

Physiological effets of PXR

Like other type II nuclear receptors, when activated, it forms a heterodimer with the retinoid X receptor, and binds to hormone response elements on DNA which elicits expression of gene products.

One of the primary targets of PXR activation is the induction of CYP3A4, an important phase I oxidative enzyme that is responsible for the metabolism of many drugs. In addition, PXR up regulates the expression of phase II conjugating enzymes such as glutathione S-transferase and phase III transport uptake and efflux proteins such as OATP2 (SLCO2A1)and MDR1(ABCB1).

Potential applications

Human PXR LBD can be used to assemble heterogenous Nuclear Receptors. With the addition of PXR ligands, any kind of genes can be activated depending on the fused DBD.

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