TABLE 3.
KD values obtained either from [3H]cytisine saturation (S) radioligand binding or [3H]cytisine homologous competition (HC) experiments are reported for different AcAChBP mutants
Binding curves for these proteins to cytisine are provided in supplemental Fig. S3 and S4.
| Mutant | KD | Method |
|---|---|---|
| nm | ||
| Wt | 222 ± 35 | HC |
| Y53W | 5.5 ± 0.5 | S |
| Y53W/I116L | 38 ± 7 | HC |
| G149K | 40 ± 9 | HC |
| Y53W/G149K | 3.9 ± 0.3 | S |
| Y53W/D75K | 9 ± 1 | S |
| Y53W/M114F | 21 ± 6 | HC |
| Y53W/I116L/G149K | 10 ± 2 | S |
| Y53W/I116L/D75K | 100 ± 15 | HC |
| Y53W/D75T | 14 ± 2 | HC |
| Y53W/I116L/D75T | 193 ± 17 | HC |
| Y53W/I116L/M114Q | 200 ± 30 | HC |
| Y53W/I116L/V106L | 56 ± 6 | HC |
| Y53W/I116L/D75T/M114Q | 186 ± 11 | HC |