Chiglitazar Preferentially Regulates Gene Expression via Configuration-Restricted Binding and Phosphorylation Inhibition of PPARγ

Figure 2

Chiglitazar preferentially induced ANGPTL4 and PDK4 expression via both PPARγ and PPARδ. Human hepatic L-02 cells were cotransfected with plasmids expressing the three PPAR subtypes or an empty vector and hRXR. At 48 hours after transfection, cells were incubated with 1 μM of each agonist or the vehicle control (0.1% (vol/vol) DMSO) for 24 hours. The mRNA level of each target gene was determined by real-time RT-PCR as described in Materials and Methods. Induced expression changes of ANGPTL4 (a), PDK4 (b), CD36 (c), and LIPE (d) were evaluated by comparison against the vehicle control. Data represent the average and standard deviation of three independent experiments. represents statistically significant differences in expression induction by Chi relative to Ros and Pio ().

(a)

(b)

(c)

(d)