Fig. 1.

Gal4 nuclear receptor profiling of T0901317. RORα and RORγ transactivation is repressed by T0901317 in a GAL4 NR library selectivity panel. Gal4 NR clones were reverse-transfected with a UAS reporter construct into HEK293T cells. After 24 h, the LXRα agonist T0901317 (2 μM final concentration) or DMSO was added and incubated for 20 h. The luciferase activity of each construct was measured and normalized to the mock (vector alone), then the -fold change in signal compared with DMSO was calculated (n = 6). Inset, HEK293T-transfected cells were separately treated with either 1 or 10 μM T0901317 or vehicle for 20 h followed by luciferase activity measurement (data shown is mean ± S.E.M., n = 6). Horizontal dashed lines represent ±5 S.D. of the control (mock transfected).