Table 6.
Intrinsic activity values of GR agonists for the induction of p57kip2, GILZ, PDK4 and CRISPLD2 in 2× GRE BEAS-2B reporter cells and the effect of indacaterol
| Glucocorticoid | Intrinsic activity (FF = 1)a | |||||||
|---|---|---|---|---|---|---|---|---|
| p57kip2 | GILZ | PDK4 | CRISPLD2 | |||||
| −Indacaterol | +Indacaterol | −Indacaterol | +Indacaterol | −Indacaterol | +Indacaterol | −Indacaterol | +Indacaterol | |
| Fluticasone furoate (100 nM) | 1.00 | 1.00 | 1.00 | 1.00 | 1.00 | 1.00 | 1.00 | 1.00 |
| Dexamethasone (1 μM) | 0.89 | 0.92 | 0.73 | 0.77 | 0.51 | 0.61 | 0.94 | 1.07 |
| GSK 9027 (3 μM) | 0.67 | 0.78 | 0.83 | 0.89 | 0.40 | 0.47 | 1.23 | 1.39 |
| Des-ciclesonide (100 nM) | 0.74 | 0.64 | 0.78 | 0.67 | 0.24 | 0.27 | 1.27 | 1.19 |
| GW 870086X (1 μM) | 0.53 | 0.62 | 0.72 | 0.76 | 0.15 | 0.15 | 1.20 | 1.37 |
| Mifepristone (1 μM) | 0.02 | 0.05 | 0.02 | 0.02 | 0.04 | 0.03 | 0.03 | 0.20 |
| Org 34517 (1 μM) | 0.02 | 0.04 | 0.01 | 0.01 | 0.02 | 0.01 | 0.08 | 0.17 |
Each GR agonist was used at a concentration that maximally activated the 2× GRE reporter. For each gene, data are expressed relative to the fold induction produced by FF, which was assigned a value of 1. Indacaterol was used at a concentration of 100 nM and added concurrently with the GR ligand.
Intrinsic activity values calculated from the data shown in Figure 6. Effects produced by indacaterol alone have been subtracted.