Fig. 6: PFM037 interferes with LXR activity. | Cell Death & Disease

Fig. 6: PFM037 interferes with LXR activity.

From: Harnessing the reverse cholesterol transport pathway to favor differentiation of monocyte-derived APCs and antitumor responses

Fig. 6

A, B Analysis of luciferase-based LXRα (A) and LXRβ (B) activation induced by PFM037, or 22R-HC used as control. Mean and s.d. of three independent experiments. ****P < 0.0001 (Anova). (C-D) Luciferase-based LXRα assays displaying the antagonistic activity of 25-HC-3S (C) and PFM037 (D). Mean and s.d. of 2 independent experiments. LXRα activation was induced by 5 (C) or 10 μM (D) of 22R-HC, 25-HC-3S was used at 25, 10, 5 and 1 μM, whereas PFM037 at 50, 25, 10, 5 and 1 μM. RLA, Relative Luciferase Activity. E Luciferase-based LXRβ assays displaying the antagonistic activity of PFM037. Mean and s.d. of 2 experiments. LXRβ activation was induced by 10 μM of 22R-HC, PFM037 was used at 50, 25, 10, 5 and 1 μM. RLA, Relative Luciferase Activity. F Luciferase-based LXRα assays to test the antagonistic activity of the inactive oxysterol 22S-HC. 22S-HC does not antagonize LXR activation induced by 5 μM of 22R-HC. 22S-HC was used at 25, 10, 5 and 1 μM. RLA, Relative Luciferase Activity. G Analysis of the expression of the LXR target genes ABCA1, SREBP1c, FASN and SCD1 following T0901317 (T1317) or PFM037 treatment. Mean and s.d. of three independent experiments. *P < 0.05; **P < 0.01; ***P < 0.001; ****P < 0.0001 (Anova). H Mammalian two-hybrid assay in Huh7 cells using Gal4-DBD-tagged RAP250-Del4 (containing NR-box1), together with pVP16-LXRα-LBD or pVP16-LXRβ-LBD, and the reporter plasmid pUAS-tk-Luc. Values shown are the mean and s.d. of two experiments performed in triplicate with luciferase activity normalized to protein content and with the activity of respective pVP16-fusion without ligand set to 1.0. The ligands 22R-HC and PFM037 was used at 10 µM when indicated. **P < 0.01; ***P < 0.001 (Anova).

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