Table 1.
Arrestin recruitment: requirement for overexpressed GRK2
| Receptor | Arrestin Recruitment | |||
|---|---|---|---|---|
| + GRK2a | No GRK2 | |||
| −LogEC50 | Emax (% of WT+GRK2) |
−LogEC50 | Emax (% of WT+GRK2) |
|
| D2L-WT | 7.69 ± 0.05 | 100 ± 2 | 6.85 ± 0.05††† | 59 ± 4††† |
| D2L-I212F | 8.06 ± 0.03** | 56 ± 1*** (−44%) | 7.22 ± 0.08**,††† | 16 ± 1***,††† (−73%) |
| D2S-WT | 7.83 ± 0.01 | 100 ± 3 | 7.20 ± 0.13††† | 59 ± 2††† |
| D2S-I212F | 8.24 ± 0.04** | 73 ± 2*** (−27%) | 7.59 ± 0.09*,††† | 21 ± 0.4***,††† (−66%) |
Quinpirole potency is shown as −logEC50. Emax was calculated by subtracting basal response from maximal response at 10 min after adding the substrate coelenterazine h, and is shown as the percentage of D2-WT with added GRK2. For D2-I212F, the percent reduction compared to the corresponding D2-WT Emax is included in parentheses. N = 3–4 independent experiments for each condition. Data are presented as mean ± SEM.
From the dataset described in van der Weijden et al. (8), except after 10 min instead of 20 min of agonist stimulation. Statistical differences were calculated by 2-way ANOVA followed by Turkey’s post-hoc test (*p<0.05, **p<0.01, ***p<0.001 compared to D2-WT; †††p<0.001 compared to the corresponding +GRK2 condition).