Table 2.
Binding affinities of CCL3 and small-molecule antagonists on CCR5 WT and mutants
| Bmax ± SEM | CCL3 | TAK-779 | Aplaviroc | |||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Residue | % of WT | log Kd ± SEM | Fold Kd | (n) | log Ki ± SEM | Fold Ki | (n) | log Ki ± SEM | Fold Ki | (n) |
| CCR5 WT | 100 ± 0.00 | −8.4 ± 0.06 | 1.0 | (19) | −7.6 ± 0.05 | 1.0 | (15) | −7.3 ± 0.03 | 1.0 | (15) |
| I116A | 63 ± 16* | −7.9 ± 0.09 | 2.7** | (4) | NT | −6.9 ± 0.02 | 2.3** | (2) | ||
| L203F | 82 ± 14 | −8.6 ± 0.10 | 0.49** | (4) | −7.7 ± 0.05 | 0.94 | (3) | −7.1 ± 0.02 | 1.4 | (3) |
| L203F+G286F | 38 ± 11** | −9.0 ± 0.34 | 0.21*** | (3) | −7.0 ± 0.21 | 4.5** | (3) | −6.8 ± 0.26 | 2.8** | (3) |
Bmax values were calculated from the homologous binding curves.
Significant change from WT calculated by Student's unpaired t-test,
*
P < 0.1,
**
P < 0.05,
***
P < 0.001.
NT, not tested.