Table 2.
Receptor activation profiles after receptor labeling by peptide‐templated acyl transfer. Wild type (wt) ETAR/ETBR‐GFP, Cys‐P1/P3‐ETAR‐GFP or Cys‐P1/P3‐ETBR‐GFP activation was assessed by Ca2+ flux analyses before (untreated) and after fluorescent labeling (labeled; n≥3 performed in duplicates). Signal transduction data were normalized to the wt receptors and represent the mean over all assay repetitions.
|
Receptor |
ETAR |
ETBR |
|||||
|---|---|---|---|---|---|---|---|
|
N‐terminal tag |
EC50 [nM] |
pEC50 ±SEM |
Emax [%] ±SEM |
EC50 [nM] |
pEC50 ±SEM |
Emax [%] ±SEM |
|
|
wt |
untreated |
2.5 |
8.6±0.07 |
105±3 |
1.1 |
8.9±0.07 |
99±2 |
|
labeled |
2.0 |
8.7±0.07 |
106±3 |
0.8 |
9.1±0.07 |
106±3 |
|
|
Cys‐P1 |
untreated |
2.6 |
8.6±0.15 |
89±6 |
0.9 |
9.1±0.17 |
108±7 |
|
labeled |
2.5 |
8.6±0.11 |
84±4 |
0.7 |
9.2±0.17 |
119±7 |
|
|
Cys‐P3 |
untreated |
2.0 |
8.7±0.13 |
113±6 |
0.7 |
9.1±0.10 |
112±4 |
|
labeled |
1.7 |
8.8±0.10 |
118±5 |
0.5 |
9.3±0.18 |
126±6 |
|