Table 5. Ligand potency (EC50 value) and efficacy (Emax value) for GCRPR, GLP1R, and chimeric receptors.
chGCRPR | chGLP1R | chimeric chGCRPR/chGLP1R | chimeric chGCRPR/huGLP1R | |||||
peptides | EC50 | Emax | EC50 | Emax | EC50 | Emax | EC50 | Emax |
[nM] | [foldinduction] | [nM] | [foldinduction] | [nM] | [foldinduction] | [nM] | [foldinduction] | |
chGCRP | 0.32±0.06 | 5.56±0.09 | 8.03±0.60 | 19.16±0.19 | 8.57±0.87 | 7.30±0.09 | 9.44±1.31 | 62.88±1.27 |
chGLP1 | 18.28±1.76a | 5.80±0.07 | 0.20±0.03a | 28.23±0.39a | 1.52±0.13a | 12.64±0.13a | 2.29±0.44a | 91.94±2.18a |
[GQA]GCRP | 0.28±0.05b | 5.60±0.09 | 0.94±0.13a | 18.99±0.30b | 0.63±0.06a | 7.18±0.07b | 0.86±0.14a | 60.62±1.15b |
[KMK]GLP1 | 1.02±0.19b | 5.77±0.10 | 0.50±0.06a | 28.38±0.39a | 1.71±0.14a | 12.77±0.12a | 3.25±0.48a | 91.15±1.65a |
Results are presented as mean ± S.E. of at least three independent experiments. a, P<0.05 vs. chGCRP; b, P<0.05 vs. chGLP1.