Table 2 Summary of cAMP assay pEC50 values for CTR ECD alanine mutants at the AMY1(a) receptor (CT(a)/RAMP1) when stimulated with rAmy (rat amylin) or hαCGRP
From: An allosteric role for receptor activity-modifying proteins in defining GPCR pharmacology
AMY 1(a) | rAmy | hαCGRP | ||||
|---|---|---|---|---|---|---|
Mutant | pEC 50 WT | pEC 50 mutant | Fold shift | pEC 50 WT | pEC 50 mutant | Fold shift |
G44A | 9.42±0.33 (5) | 9.65±0.35 (5) | 9.98±0.06 (3) | 10.13±0.16 (3) | ||
R45A | 9.35±0.29 (5) | 9.44±0.25 (5) | 9.69±0.33 (3) | 9.67±0.31 (3) | ||
M48A | 9.51±0.21 (4) | 9.35±0.13 (4) | 9.52±0.26 (4) | 9.22±0.32 (4) | ||
W79A | 9.84±0.25 (6) | 7.88±0.27 (6)*** | 91 | 9.43±0.25 (6) | 7.46±0.25 (6)*** | 93 |
F99A | 9.90±0.08 (5) | 9.18±0.23 (5)* | 5 | 10.19±0.12 (5) | 9.04±0.26 (5)** | 14 |
D101A | 10.05±0.18 (6) | 8.22±0.15 (6)*** | 68 | 9.74±0.28 (6) | 6.90±0.17 (6)*** | 692 |
F102A | 9.67±0.24 (5) | 7.81±0.09 (5)*** | 72 | 9.74±0.18 (4) | 6.79±0.19 (4)*** | 891 |
H121A | 9.73±0.18 (5) | 9.12±0.09 (5)* | 4 | 9.62±0.15 (5) | 8.60±0.14 (5)** | 11 |
N124A | 9.74 ±0.19 (4) | 9.58±0.19 | 9.31±0.26 (5) | 9.02±0.13 (5) | ||
R126A | 9.35±0.28 (4) | 8.48±0.18 (4)* | 7 | 9.48±0.34 (4) | 8.37±0.17 (4)* | 13 |
W128A | 9.90±0.14 (4) | 8.00±0.18 (4)*** | 79 | 9.84±0.26 (4) | 7.26±0.16 (4)*** | 380 |
Y131A | 9.74±0.28 (4) | 8.47±0.26 (4)* | 19 | 10.11±0.18 (4) | 8.64±0.29 (4)** | 30 |
