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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 (R 2 =0.4; P&lt;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&lt;0.01).

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