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

Figure 5

Increased ANGPTL4 and PDK4 expressions are associated with inhibition of TNFα-induced and CDK5-mediated phosphorylation of PPARγ. HPA-v cells were incubated with different protein kinases (i.e., VEGFR and PDGFR inhibitor Sutent (1 μM), AURK A/B/C inhibitor VX680 (0.1 μM), MEK1/2 inhibitor U0126 (1 μM), and CDK5 inhibitor roscovitine (Rosc, 10 μM) or vehicle control (0.1% (vol/vol) DMSO) in the presence of TNFα (5 ng/ml) for 24 hours. Total RNA was extracted and subjected to real-time RT-PCR as described in Materials and Methods. Data represent the average and standard deviation of three independent experiments. represents statistically significant differences in expression induction by roscovitine compared to all other inhibitors ().

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