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

Figure 1

Preferential induction of ANGPTL4 and PDK4 mRNA and protein by chiglitazar. (a) and (b) Human preadipocyte HPA-v cells were incubated with different concentrations of the three agonists for 24 hours before total RNA was collected and purified. Real-time RT-PCR was performed as described in Materials and Methods. The dose-dependent changes in ANGPTL4 (a) and PDK4 (b) expression induced by the different agonists were normalized against the sample treated with vehicle (0.01% (vol/vol) DMSO) only. (c) HPA-v cells were incubated with 1 μM of each agonist for 48 hours. Protein levels were assessed by immunoblot analysis using the respective primary antibodies (β-Actin, 1 : 1000; LIPE, 1 : 1000; CD36, 1 : 1000, PDK4, 1 : 500; ANGPTL4, 1 : 500) as described in Materials and Methods. Chi: chiglitazar; Ros: rosiglitazone; Pio: pioglitazone; LIPE: lipase, hormone-sensitive (HSL). 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 ().

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