Table 3.
Table showing relative agonist efficacies and potencies of the ligands for transrepression via the GR on AP-1 or NFκB cis-elements and the IL6 gene*
| Transrepression | ||||||
|---|---|---|---|---|---|---|
| COS-1 | PBMC | |||||
| AP-1 | NFκB | IL6 | ||||
| Ligand | MAX (%) ± SEM | EC50 (M) ± SEM | MAX (%) ± SEM | EC50 (M) ± SEM | MAX (%) ± SEM | EC50 (M) ± SEM |
| DEX | 100 ± 0.0a | 7.24 ± 1.57 × 10−14a | 100 ± 0.0a | 1.08 ± 0.38 × 10−14a | 100 ± 9.16a | 7.63 ± 6.31×10−9a |
| MPA | 96.94 ± 4.60a | 2.49 ± 0.64 × 10−11b | 84.46 ± 4.92a | 2.84 ± 1.88 × 10−14a, c | 101.62 ± 11.50a | 0.92 ± 1.45×10−8a |
| NET | 33.86 ± 9.97b | 3.58 ± 2.85 × 10−9 #c | 32.63 ± 9.86b | 8.35 ± 5.65 × 10−13# a,b,c | 57.95 ± 9.55$a | 4.66 ± 4.32×10−9$a |
| LNG | 39.60 ± 4.31b | 3.32 ± 2.89 x 10−10 #b,c | 38.04 ± 9.70b | 5.00 ± 3.00 × 10−13# a,b,c | 88.53 ± 14.82a | 2.95 ± 6.27×10−8a |
| ETG | 79.60 ± 7.27a | 2.90 ± 0.99 × 10−10b,c | 81.65 ± 7.32a | 6.04 ± 3.49 × 10−11b | 77.19 ± 17.00a | 2.44 ± 0.10×10−8a |
| NES | 92.03 ± 4.39a | 5.41 ± 3.06 × 10−10b,c | 85.66 ± 8.58a | 3.49 ± 2.05 × 10−11b,c | 100.13 ± 7.92a | 5.49 ± 5.82×10−9a |
Data shown in Fig. 2C-E, were analyzed to obtain the MAX (%) ± SEM and EC50 (M) ± SEM, values for each ligand for the GR.
The EC50 values for NET and LNG should be interpreted with caution as very weak agonist activity was observed.
The MAX and EC50 values for NET should be interpreted with caution as Prism 9 deemed this curve unstable due to variable data.
Statistical significance between treatment groups was determined using one-way ANOVAs with Tukey post-test.