Fig. 2.

Activation of hCAR3 and hCAR1+A by prototypical hCAR activators. HepG2 cells were transfected with CYP2B6-PBREM reporter, and hCAR3 or hCAR1+A expression vectors as described under Materials and Methods.7, Transfected cells were subsequently treated with vehicle control (0.1% DMSO) or CITCO at the concentration of 0.1, 1.0, and 5.0 μM (A); or with known hCAR activators, including PB, ART, PHN, EFV, and NVP, at indicated concentrations for 24 h (B). RIF (10 μM) was included as non-hCAR activator. After harvesting cell lysates, luciferase activities were determined and expressed relative to hCAR3 vehicle control. Data represent the mean ± S.D. (n = 3) (**, p < 0.01 denotes comparison between hCAR1+A and hCAR3 for each paired group, respectively).