TABLE 1.
Affinity, potency and efficacy values of the N‐terminal truncated GLP‐2 variants on the GLP‐2R
| Competition binding | cAMP activation | cAMP inhibition | |||||
|---|---|---|---|---|---|---|---|
| Log IC50 ± SEM | Ki (nM) | Log EC50 ± SEM | EC50 (nM) | Emax ± SEM (%) | Log IC50 ± SEM | IC50 (nM) | |
| GLP‐2(1‐33) | −8.7 ± 0.12 | 2.2 | −10.2 ± 0.14 | 0.06 | 100 ± 4.7 | ‐ | ‐ |
| GLP‐2(2‐33) | −8.1 ± 0.11 | 7.9 | −8.1 ± 0.50 | 7.9 | 20 ± 3.2 | −6.8 ± 0.34 | 174 |
| GLP‐2(3‐33) | −8.1 ± 0.13 | 8.1 | −7.6 ± 0.26 | 25 | 21 ± 2.2 | −6.7 ± 0.39 | 204 |
| GLP‐2(4‐33) | −8.2 ± 0.16 | 6.5 | −6.8 ± 0.30 | 158 | 17 ± 2.6 | −7.1 ± 0.18 | 79 |
| GLP‐2(5‐33) | −7.9 ± 0.15 | 12 | −7.6 ± 0.24 | 25 | 40 ± 4.1 | −6.7 ± 0.34 | 200 |
| GLP‐2(6‐33) | −7.5 ± 0.11 | 33 | −7.4 ± 0.24 | 40 | 46 ± 5.1 | −6.3 ± 0.71 | 490 |
| GLP‐2(7‐33) | −7.7 ± 0.15 | 22 | −6.9 ± 0.24 | 126 | 27 ± 3.8 | No inhibition | |
| GLP‐2(8‐33) | −7.1 ± 0.12 | 81 | −7.2 ± 0.31 | 63 | 19 ± 3.0 | No inhibition | |
| GLP‐2(9‐33) | −7.1 ± 0.15 | 81 | −6.7 ± 0.08 | 200 | 65 ± 3.6 | No inhibition | |
| GLP‐2(10‐33) | −6.9 ± 0.19 | 123 | No activation | −6.39 ± 0.66 | 398 | ||
| GLP‐2(11‐33) | −6.1 ± 0.53 | 871 | No activation | No inhibition | |||
Note: The table displays a summary of the affinity, potency and efficacy values of the N‐terminal truncated GLP‐2 variants on the human GLP‐2R tested in the binding and cAMP accumulation experiments. The values originate from the data shown in Figures 1 and 2 from n = 3 independent experiments carried out in duplicate.