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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

ER-DBD can be fused with various LBDs in order to get heterogenous composite Nuclear Receptors. With addition of the LBD's ligand the receptor can bind to Estrogen Receptor Response element and activate downstream gene expression.

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