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. Author manuscript; available in PMC: 2012 Jun 17.
Published in final edited form as: ACS Chem Biol. 2011 Mar 17;6(6):618–627. doi: 10.1021/cb100396s

Figure 1.

Figure 1

A) Synthetic non-retinoid pan-RAR inverse agonist SR-03000000065. B) Gal4 nuclear receptor profiling of SR-0065. RARα, RARβ and RARγ transactivation is repressed by SR-0065 in a Gal4 NR library selectivity panel. A UAS luciferase reporter construct was reverse-transfected into HEK293T cells along with Gal4 NR clones or a Gal4-VP16 clone as a constitutively active positive control. After 4 hours, cells were treated with 5μM SR-0065 or DMSO only and incubated for 20 hours. The luciferase activity of each construct was measured and normalized first to the DMSO only treated samples, then the fold change in signal of each NR construct compared to the constitutively active Gal4-VP16 was calculated (n=3).