TABLE 3.
Gq or Gs signaling of the WT GHSR, B2AR, and GPPR119 and the AspII:10Glu mutant variant of these receptors
The constructs were expressed in transiently transfected COS-7 cells. The constitutive and ghrelin-induced Gq signaling was determined for the ghrelin receptor, whereas signaling through the Gs signaling pathway was determined for B2AR (pindolol) and GPR119 (AR-231453). The Emax values are expressed as percentage of the ligand-induced signaling for the WT receptors. Values are shown ± S.E. CA means constitutive activity.
| Construct | Expression level | n | CA | EC50(nm) (ligand) | Emax | n |
|---|---|---|---|---|---|---|
| GHSR 1a WT | 1 ± 0.02 | 3 | 43.4 ± 2.06 | 0,36 ± 0.27 (Ghrelin) | 100 | 3 |
| AspII:10Glu | 0.60 ± 0.06 | 3 | 3 | |||
| B2AR WT | 1 ± 0.03 | 5 | 9.9 ± 2.55 | 2.97 ± 1.09 (Pindolol) | 100 | 6 |
| AspII:10Glu | 0.68 ± 0.06 | 5 | 2 ± 1.92 | 5.68 ± 2.90 | 16.6 ± 5.35 | 5 |
| GPR119 WT | 1 ± 0.09 | 5 | 43.6 ± 3.43 | 2.22 ± 0.34 (AR-231453) | 100 | 5 |
| AspII:10Glu | 0.51 ± 0.11 | 5 | 27.5 ± 5.3 | 17.0 ± 5.01 | 56 ± 5.01 | 5 |