Figure 2.
TR-FRET-based PPARα/δ/γ-LBD coactivator recruitment assay. (A–C) Control experiments. Human PPARα/δ/γ-LBD-mediated recruitment of coactivator peptides, PGC1α (filled symbols) and SRC1 (open symbols), was induced by selective PPAR agonists, GW7647 for PPARα (A), GW501516 for PPARδ (B), and GW1929 for PPARγ (C) in a concentration-dependent manner. Their maximal responses at 1 µM are used as the 100% responses in (D–I). (D–I) PPARα/δ/γ-LBD-mediated PGC1α (D–F) and SRC1 (G–I) coactivator peptide recruitment was induced by bezafibrate (D,G), fenofibric acid (E,H), and pemafibrate (F,I) in a concentration-dependent manner. Data are means ± SE of 3–4 independent experiments with duplicate samples, and calculated EC50 values are shown.