Table 2 Summary of pharmacological parameters measured for apelin receptor variants
Variant | Expression | Fl. ligand binding | Radioligand binding | Function | |||||
---|---|---|---|---|---|---|---|---|---|
Mem. eGFP (% WT) | Object count/ region | Mem. apelin647 (% WT) | Mem. ELA647 (% WT) | KD (nM) | Bmax (fmol/ mg) | Hill slope (nH) | pD2 | Emax (ΔPWV) | |
WT | 100.00 ± 23.52 | 17.00 ± 6.88 | 100.0 ± 27.09 | 100.00 ± 19.10 | 0.21 ± 0.05 | 236.80 ± 27.07 | 1.26 ± 0.22 | 8.32 ± 0.24 | 39.48 ± 3.93 |
V/L381.42 | 121.40 ± 31.87 | 16.58 ± 7.99 | 94.74 ± 17.52 | 92.53 ± 28.43 | NBD | NBD | NBD | 7.67 ± 0.48 | 42.55 ± 15.16 |
G/X451.49 | 32.18 ± 16.67 | 7.67 ± 3.68 | 12.18 ± 6.48 | 20.73 ± 12.55 | NBD | NBD | NBD | – | – |
T/M892.64 | 104.94 ± 34.40 | 19.83 ± 8.67 | 82.95 ± 24.46 | 31.75 ± 13.20 | 0.25 ± 0.04 | 440.47 ± 38.36 | 1.55 ± 0.22 | 7.72 ± 0.21 | 50.06 ± 8.32 |
R/H1684.64 | 119.93 ± 40.29 | 23.00 ± 10.04 | 2.53 ± 2.10 | 17.29 ± 9.42 | NBD | NBD | NBD | n/a | 5.49 ± 6.42 |
T/X2275.64 | 12.38 ± 3.90 | 5.08 ± 1.51 | 2.94 ± 2.78 | 14.83 ± 7.02 | NBD | NBD | NBD | – | – |
Untrans. | 0.00 | 0.00 | 0.00 | 0.00 | NBD | NBD | NBD | n/a | 0.21 ± 7.07 |