Figure 1.

PPARα/δ/γ-LBD-mediated transactivation assay in COS-7 cells. (A–C) Control experiments. Human PPARα/δ/γ-LBD-mediated Firefly luciferase transactivation was induced by selective PPAR agonists: GW7647 for PPARα (A), GW501516 for PPARδ (B), and GW1929 for PPARγ (C) in a concentration-dependent manner. The maximal responses were observed at 0.1 µM, 0.02 µM, and 1 µM, respectively, which are used as the 100% responses in (E–G). (D) Chemical structures of fibrates used in this study. Fenofibrate is a prodrug that is metabolized by tissue and plasma carboxylesterases [22] to its active form, fenofibric acid. (E–G) PPARα/δ/γ-LBD-mediated transactivation by bezafibrate (E), fenofibric acid (F), and pemafibrate (G). Data are means ± standard error (SE) of three independent experiments with duplicate samples, and calculated EC₅₀ values are shown.