Table 3.
Potency of FFA2 agonists in the TGFα shedding assay and effects of Lys65Xaa mutations.
| Cells | Agonist | WT | K65R | K65A | K65E |
|---|---|---|---|---|---|
| Parental | C3 | 4.93 ± 0.04 | 4.68 ± 0.09 | 2.23 ± 0.13*** | 2.79 ± 0.07*** |
| Compound 1 | 8.12 ± 0.08 | 8.14 ± 0.03 | 6.88 ± 0.04*** | 6.88 ± 0.04*** | |
| ΔGq/11 | C3 | 4.40 ± 0.07aaa | 3.98 ± 0.04* | 2.67 ± 0.17*** | 2.39 ± 0.07*** |
| Compound 1 | 7.84 ± 0.08a | 7.51 ± 0.10 | 6.02 ± 0.11*** | 5.94 ± 0.08*** | |
| ΔG12/13 | C3 | 4.38 ± 0.10aaa | 4.11 ± 0.09 | 2.14 ± 0.08*** | 2.52 ± 0.05*** |
| Compound 1 | 7.49 ± 0.08aaa | 7.33 ± 0.11 | 6.23 ± 0.11*** | 6.16 ± 0.13*** |
Values represent pEC50 of agonists in denoted cell lines. Data are mean ± SEM with n ≥ 3. */ap ≤ 0.05. **/aap ≤ 0.01. ***/aaap ≤ 0.001. One-way analysis of variance was followed by Dunnett’s test with WT (*) or parental cells (a) as reference.