Figure 3.

Activation profile of hPAR in transiently transfected Caco-2 cells. (A) Caco-2 cells were transfected with luciferase reporter plasmid and expression plasmid encoding GAL4-hPAR chimeric protein. Cells then were treated with vehicle (DMSO) or 10 μM of the indicated compounds for 24 hr. Cell extracts were analyzed for luciferase activity, and data represent the mean ± SD. ∗∗, P < 0.001 (Student’s t test) as compared with the DMSO control. (B) Caco-2 cells were transfected with luciferase reporter plasmid and expression plasmid encoding GAL4-hPAR chimeric protein. Cells then were treated with the indicated concentration of clotrimazole (solid circles), 3α-hydroxy-5β-pregnane-11,20,dione, methanesulfonate (open diamonds), Rifampicine (solid triangles), or Nifidipine (asterisks) for 24 hr. Cell extracts were analyzed for luciferase activity, and data are plotted as the percentage of maximal induction.