Part:BBa_K364325:Experience

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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 function 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).

Possible applications of GAL4-PXR

By the addition of lipid ligand, the created system activates the expression of any kind of genes fused to UAS(upstream activation seqence)previously. Also can be used as a lipid sensor by activating reporter genes (e.g. Luciferase).

Applications of BBa_K364325

Picture of gel electrophoresis: Gal4-PXR in pCDNA3.1 resulting an insert of 1181 bp.

Picture of Western blot: Gal4-PXR composite construct is highly expressed after transferring it into pCDNA3.1

User Reviews

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