ERRγ inverse agonist GSK5182 down-regulates the hypoxia-induced PDK4 expression.

Abstract

<p>(<b>A–B</b>) HepG2 cells were transfected with hPDK4-Luc. After transfection, the cells were exposed in hypoxia and treated with or without GSK5182. Harvested lysates were utilized for luciferase and β-galactosidase assay (A). Q-PCR was performed using isolated total RNA (B). Experiments were done in triplicate and data are expressed as the fold activation relative to the control. (<b>C</b>) HepG2 cells were seeded in 60-cm<sup>2</sup> dishes and incubated overnight. The cells were incubated in hypoxia and treated with or without GSK5182. Total protein was harvesed for Western blot analysis using indicated antibodies. (<b>D</b>) HepG2 cells were seeded in 60-cm<sup>2</sup> dishes and incubated overnight. The cells were treated with or without chemicals (DFO and GSK5182) for 6 hr. Total protein and mRNA were isolated for Western blot assay and RT-PCR and normalized with α or β-tubulin and β-actin. (<b>E</b>) A schematic representation. All data are representative of at least three independent experiments. Error bars show ± S.E.M. <sup>**</sup><i>P</i><0.01, <sup>***</sup><i>P</i><0.001 by two-tailed Student <i>t</i>-test.</p

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