Expression of Pregnane-X-Receptor Transcript in Peripheral Blood Mononuclear Cells and Correlation with Mdr1 Mrna

P-glycoprotein (P-gp) limits bioavailability and accumulation of HIV protease inhibitors (PIs). PIs are ligands for the pregnane-X-receptor (PXR), which regulates P-gp expression. This occurs when ligands activate the receptor, initiating binding to response elements in the MDR1 promoter. PXR also activates cytochrome P4503A4 (CYP3A4) and a correlation between hepatic PXR and CYP3A4 mRNA has been reported. We have examined the relationship between MDR1 and PXR mRNA in peripheral blood cells and demonstrate a significant correlation in 18 volunteers (R2=0.4; P<0.005). PXR was approximately 250-fold lower in peripheral blood mononuclear cells than in liver (1.6 ±1.2 vs 450 ±298; n=6; P<0.01).

• Publication year

  2004

• Venue

  Antiviral Therapy

• Publication date

  2004-07-01

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1177/135965350400900510PMID 15535420
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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