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. 2015 Mar 24;172(10):2634–2653. doi: 10.1111/bph.13087

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.

a

Intrinsic activity values calculated from the data shown in Figure 6. Effects produced by indacaterol alone have been subtracted.