Table 1.
Expression level and functional analyses of agonists on CCR5 WT and mutants as measured in PI turnover and β-arrestin recruitment
| PI turnover | β-Arrestin recruitment | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Expression level | Constitutive activity (%) | Emax | CCL3 | CCL5 | Constitutive activity (%) | Emax | CCL3 | CCL5 | ||||||||||
| Residue | % of WT ± SEM | (basal/Emax) × 100 | % of WT ± SEM | log EC50 ± SEM | Fold EC50 | (n) | log EC50 ± SEM | Fold EC50 | (n) | (basal/Emax) × 100 | % of WT ± SEM | log EC50 ± SEM | Fold EC50 | (n) | log EC50 ± SEM | Fold EC50 | (n) | |
| CCR5 WT | 100 ± 0.00 | 1.6 ± 1.8 | 100 ± 0.00 | −8.1 ± 0.07 | 1.0 | (41) | −9.1 ± 0.07 | 1.0 | (37) | 29 ± 2.2 | 100 ± 0.00 | −8.1 ± 0.08 | 1.0 | (40) | −8.4 ± 0.24 | 1.0 | (8) | |
| I116A | 102 ± 6.0 | 27 ± 3.3*** | 97 ± 16 | −8.1 ± 0.28 | 1.1 | (6) | −9.1 ± 0.34 | 0.93 | (4) | 52 ± 4.6** | 91 ± 13 | −7.9 ± 0.16 | 1.8 | (9) | −7.4 ± 0.41 | 9.5** | (4) | |
| L203F | 108 ± 10 | 21 ± 1.7*** | 81 ± 17 | −8.0 ± 0.09 | 1.3 | (7) | −9.2 ± 0.14 | 0.84 | (4) | 50 ± 3.0*** | 88 ± 8.5 | −8.5 ± 0.16 | 0.35** | (15) | −8.8 ± 0.22 | 0.36 | (4) | |
| L203F+G286F | 13 ± 1.7*** | 38 ± 3.1*** | 21 ± 1.5*** | −7.8 ± 0.14 | 2.0 | (4) | −9.0 ± 0.78 | 1.2 | (4) | NA | NA | NA | (9) | NA | (3) | |||
Significant change from WT calculated by Student's unpaired t-test.
**
P < 0.05,
***
P < 0.001.
NA, no activity.