The major human pregnane X receptor (PXR) splice variant, PXR.2, exhibits significantly diminished ligand-activated transcriptional regulation.

@article{Lin2009TheMH,
  title={The major human pregnane X receptor (PXR) splice variant, PXR.2, exhibits significantly diminished ligand-activated transcriptional regulation.},
  author={Yvonne S. Lin and Kazuto Yasuda and Mahfoud Assem and Cynthia Brimer Cline and Joe Barber and C. Li and Vladyslav V. Kholodovych and Ni Ai and John D. Chen and William J. Welsh and Sean Ekins and Erin G. Schuetz},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2009},
  volume={37 6},
  pages={1295-304}
}
The pregnane X receptor (PXR; PXR.1) can be activated by structurally diverse lipophilic ligands. PXR.2, an alternatively spliced form of PXR, lacks 111 nucleotides encoding 37 amino acids in the ligand binding domain. PXR.2 bound a classic CYP3A4 PXR response element (PXRE) in electrophoretic mobility shift assays, but transfected PXR.2 failed to transactivate a CYP3A4-promoter-luciferase reporter plasmid in HepG2 cells treated with various PXR ligands. Cotransfection experiments showed that… CONTINUE READING
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