Table 1 Summary of cAMP assay pEC50 values for CTR ECD alanine mutants at the CT(a) receptor when stimulated with hCT, rAmy (rat amylin) or hαCGRP
From: An allosteric role for receptor activity-modifying proteins in defining GPCR pharmacology
CT (a) | hCT | rAmy | hαCGRP | ||||||
|---|---|---|---|---|---|---|---|---|---|
Mutant | pEC 50 WT | pEC 50 mutant | Fold shift | pEC 50 WT | pEC 50 mutant | Fold shift | pEC 50 WT | pEC 50 mutant | Fold shift |
G44A | 9.77±0.15 (3) | 9.80±0.12 (3) | 8.06±0.19 (4) | 8.03±0.19 (4) | — | — | |||
R45A | 9.51±0.19 (4) | 9.47±0.32 (4) | 7.87±0.10 (4) | 7.75±0.10 (4) | — | — | |||
M48A | 9.38±0.18 (5) | 9.04±0.21 (5) | 7.96±0.08 (4) | 7.83±0.25 (4) | — | — | |||
W79A | 9.49±0.28 (4) | 8.17±0.14 (4)** | 21 | 8.26±0.15 (6) | 7.37±0.20 (6)** | 8 | 6.97±0.08 (4) | 6.35±0.16 (4)* | 4 |
F99A | 9.49±0.23 (5) | 8.64±0.12 (5)* | 7 | 8.15±0.13 (5) | 8.03±0.16 (5) | 7.06±0.15 (4) | 6.63±0.10 (4) | ||
D101A | 9.84±0.07 (5) | 8.61±0.13 (5)*** | 17 | 8.17±0.04 (6) | 8.04± 0.04 (6) | 7.14±0.15 (6) | 6.51±0.04 (6)** | 4 | |
F102A | 9.51±0.16 (7) | 7.44±0.16 (7)*** | 118 | 8.40±0.14 (5) | 7.70±0.23 (5)* | 5 | 6.99±0.08 (4) | 6.30±0.06 (4)*** | 5 |
H121A | 9.90±0.06 (5) | 9.13±0.09 (5)*** | 6 | 8.17±0.17 (5) | 7.97±0.14 (5) | 7.26±0.19 (4) | 6.58±0.04 (4)* | 5 | |
N124A | 9.83±0.31 (3) | 9.61±0.38 (3) | 8.28±0.15 (4) | 8.24±0.19 (3) | — | — | |||
R126A | 9.26±0.07 (5) | 9.57±0.17 (5) | 8.64±0.19 (5) | 8.12±0.11 (5)** | 3 | 7.79±0.16 (5) | 7.68±0.13 (5) | ||
W128A | 9.80±0.24 (6) | 7.96±0.06 (6)*** | 69 | 8.31±0.10 (5) | 8.03±0.07 (5) | 7.20±0.13 (6) | 6.74±0.19 (6) | ||
Y131A | 9.37±0.25 (5) | 8.57±0.16 (5)* | 6 | 8.40±0.19 (4) | 7.51±0.29 (4)* | 8 | 7.16±0.14 (4) | 6.51±0.11 (4)* | 5 |
