Table 1. Effect of NR3C1 ligands on 2×GRE activation in the presence and absence of TNF.
| Naive | +TNF | |||
|---|---|---|---|---|
| E max (% Dex) | pEC50 (M) | E max (% Dex) | pEC50 (M) | |
| Dexamethasone | 100 ± 3.2 | 7.6 ± 0.1 | 58.7 ± 3.2 | 7.5 ± 0.1 * |
| Fluticasone Propionate | 111.2 ± 4.3 | 8.2 ± 0.1 | 51.0 ± 2.8 | 8.2 ± 0.1 |
| Budesonide | 109.9 ± 2.6 | 8.2 ± 0.1 | 56.9 ± 2.0 | 8.1 ± 0.1 |
| Fluticasone Furoate | 108.0 ± 2.9 | 8.8 ± 0.0 | 57.8 ± 1.5 | 8.7 ± 0.0 |
| GSK9027 | 77.2 ± 1.0 | 7.1 ± 0.0 | 40.7 ± 0.9 | 7.0 ± 0.1 |
| Des-ciclesonide | 76.0 ± 2.0 | 8.6 ± 0.1 | 43.1 ± 1.0 | 8.5 ± 0.1 |
| RU24858 | 74.9 ± 1.1 | 7.4 ± 0.0 | 46.0 ± 0.8 | 7.3 ± 0.0 * |
| GW870086X | 50.1 ± 1.1 | 8.3 ± 0.1 | 29.8 ± 1.4 | 8.0 ± 0.2 * |
BEAS-2B cells harboring a 2×GRE reporter were either not treated (Naive) or were pre-treated with tumor necrosis factor (TNF; 10 ng/ml) for 1 h, prior to addition of a maximally effective concentration of the indicated NR3C1 ligands. After 6 h, cells were harvested for luciferase assay. Data are from Fig. 5 and are expressed as a percent of 1 μM dexamethasone treatment (Naïve: E Max = 6.3 ± 0.2 fold; +TNF E Max = 3.7 ± 0.2 fold). Statistical analyses were conducted by Student’s t test to compare the EC50s of the ligand in the presence and absence of TNF, as indicated: P < 0.05 *.