Transactivation of Retinoid Receptors by TT or 9CTT
| Receptor . | Reporter . | Luciferase Induction (ratio) . | |||
|---|---|---|---|---|---|
| TT . | 9CTT . | ATRA . | LGD1069 . | ||
| CMX | TK-TREpx2-LUC | 2.6 ± 0.1 | 2.4 ± 0.2 | 4.1 ± 0.3 | |
| RAR-α | 10.7 ± 1.8 | 14.0 ± 1.2 | 37.1 ± 3.9 | ||
| RAR-β | 7.1 ± 1.0 | 7.7 ± 1.0 | 11.8 ± 1.8 | ||
| RAR-γ | 7.9 ± 0.2 | 7.8 ± 0.6 | 12.7 ± 1.3 | ||
| PML/RAR-α | 3.5 ± 0.2 | 4.2 ± 0.3 | 13.3 ± 1.7 | ||
| RAR-α + PML/RAR-α | 4.0 ± 0.3 | 3.4 ± 0.5 | 13.3 ± 2.3 | ||
| RAR-β + PML/RAR-α | 2.6 ± 0.4 | 3.0 ± 0.2 | 10.4 ± 0.9 | ||
| CMX | TK-mRARβx2-LUC | 6.2 ± 1.0 | 5.5 ± 0.4 | 9.4 ± 0.5 | |
| RAR-α | 8.7 ± 0.9 | 9.0 ± 0.4 | 15.2 ± 0.4 | ||
| RAR-β | 7.9 ± 0.9 | 6.7 ± 0.2 | 10.2 ± 1.2 | ||
| RAR-γ | 3.8 ± 0.2 | 3.3 ± 0.3 | 5.5 ± 0.2 | ||
| PML/RAR-α | 2.3 ± 0.2 | 2.7 ± 0.2 | 9.0 ± 1.2 | ||
| CMX | TK-βREx3-LUC | 46.1 ± 3.2 | 47.4 ± 9.0 | 68.1 ± 22.2 | |
| PML/RAR-α | 10.6 ± 0.6 | 11.3 ± 0.4 | 38.7 ± 12.4 | ||
| GAL-RAR-α | TK-GAL4-UASx4-LUC | 94.5 ± 14.3 | 12.2 ± 2.4 | 2,648 ± 36 | |
| GAL-RAR-β | 42.6 ± 2.0 | 16.7 ± 0.7 | 119 ± 10 | ||
| GAL-RAR-γ | 15.1 ± 0.4 | 3.7 ± 0.8 | 24.0 ± 1.5 | ||
| CMX | TK-CRBPII-LUC | 1.2 ± 0.0 | 1.1 ± 0.2 | 1.4 ± 0.1 | |
| RXR-α | 1.7 ± 0.3 | 2.4 ± 0.4 | 5.9 ± 0.7 | ||
| GAL-RXR-α | TK-GAL4-UASx4-LUC | 2.1 ± 0.2 | 1.6 ± 0.1 | 70.5 ± 1.2 | |
| GAL-RXR-β | 1.7 ± 0.1 | 1.5 ± 0.1 | 59.8 ± 2.3 | ||
| GAL-RXR-γ | 2.0 ± 0.2 | 2.2 ± 0.1 | 9.4 ± 0.9 | ||
| Receptor . | Reporter . | Luciferase Induction (ratio) . | |||
|---|---|---|---|---|---|
| TT . | 9CTT . | ATRA . | LGD1069 . | ||
| CMX | TK-TREpx2-LUC | 2.6 ± 0.1 | 2.4 ± 0.2 | 4.1 ± 0.3 | |
| RAR-α | 10.7 ± 1.8 | 14.0 ± 1.2 | 37.1 ± 3.9 | ||
| RAR-β | 7.1 ± 1.0 | 7.7 ± 1.0 | 11.8 ± 1.8 | ||
| RAR-γ | 7.9 ± 0.2 | 7.8 ± 0.6 | 12.7 ± 1.3 | ||
| PML/RAR-α | 3.5 ± 0.2 | 4.2 ± 0.3 | 13.3 ± 1.7 | ||
| RAR-α + PML/RAR-α | 4.0 ± 0.3 | 3.4 ± 0.5 | 13.3 ± 2.3 | ||
| RAR-β + PML/RAR-α | 2.6 ± 0.4 | 3.0 ± 0.2 | 10.4 ± 0.9 | ||
| CMX | TK-mRARβx2-LUC | 6.2 ± 1.0 | 5.5 ± 0.4 | 9.4 ± 0.5 | |
| RAR-α | 8.7 ± 0.9 | 9.0 ± 0.4 | 15.2 ± 0.4 | ||
| RAR-β | 7.9 ± 0.9 | 6.7 ± 0.2 | 10.2 ± 1.2 | ||
| RAR-γ | 3.8 ± 0.2 | 3.3 ± 0.3 | 5.5 ± 0.2 | ||
| PML/RAR-α | 2.3 ± 0.2 | 2.7 ± 0.2 | 9.0 ± 1.2 | ||
| CMX | TK-βREx3-LUC | 46.1 ± 3.2 | 47.4 ± 9.0 | 68.1 ± 22.2 | |
| PML/RAR-α | 10.6 ± 0.6 | 11.3 ± 0.4 | 38.7 ± 12.4 | ||
| GAL-RAR-α | TK-GAL4-UASx4-LUC | 94.5 ± 14.3 | 12.2 ± 2.4 | 2,648 ± 36 | |
| GAL-RAR-β | 42.6 ± 2.0 | 16.7 ± 0.7 | 119 ± 10 | ||
| GAL-RAR-γ | 15.1 ± 0.4 | 3.7 ± 0.8 | 24.0 ± 1.5 | ||
| CMX | TK-CRBPII-LUC | 1.2 ± 0.0 | 1.1 ± 0.2 | 1.4 ± 0.1 | |
| RXR-α | 1.7 ± 0.3 | 2.4 ± 0.4 | 5.9 ± 0.7 | ||
| GAL-RXR-α | TK-GAL4-UASx4-LUC | 2.1 ± 0.2 | 1.6 ± 0.1 | 70.5 ± 1.2 | |
| GAL-RXR-β | 1.7 ± 0.1 | 1.5 ± 0.1 | 59.8 ± 2.3 | ||
| GAL-RXR-γ | 2.0 ± 0.2 | 2.2 ± 0.1 | 9.4 ± 0.9 | ||
The transactivating activity of TT and 9CTT for retinoid receptors was examined using several reporters. CV-1 cells that has been transfected with receptor plasmid and reporter plasmid were incubated with or without 10−5 mol/L TT or 9CTT for 24 hours. pCMX plasmid is an empty vector; the genes for retinoid receptors were introduced into the pCMX vector. ATRA (10−6 mol/L) and LGD1069 (10−6 mol/L) were used as positive controls for RARs and RXRs, respectively. Values are given relative to luciferase activity in unstimulated cells as 1 U and represent the means ± SD from duplicate or triplicate experiments.