Differential modulation of agonist peptides at the human GLP-1R Met149 receptor variant by compound 2 in cAMP accumulation
Data were analyzed using a three-parameter logistic equation as defined in eq. 1. pEC50 values represent the negative logarithm of the concentration of agonist that produces half the maximal response. All data are normalized to the response elicited by 10−7 M forskolin and are mean ± S.E.M. of three to five independent experiments, conducted in duplicate.
| pEC50 | ||||
|---|---|---|---|---|
| Wild Type | Met149 | |||
| Peptide | + 3 μM Compound 2 | Peptide | + 3 μM Compound 2 | |
| GLP-1(7–36)NH2 | 10.2 ± 0.3 | 10.8 ± 0.6 | 7.0 ± 0.2 | 9.7 ± 0.8* |
| Exendin-4 | 10.4 ± 0.2 | 10.8 ± 0.6 | 8.5 ± 0.2 | 9.6 ± 0.7† |
| Oxyntomodulin | 8.9 ± 0.2 | 9.8 ± 1.0† | N.D. | N.D. |
N.D., data unable to be experimentally defined or with incomplete curves.
* Statistically significant, P < 0.05 compared with peptide control, paired t test.
† P = 0.05 compared with peptide control, paired t test.