TABLE 4.
Summary of expression, binding and signaling results for β-strand 5 mutants in HEK 293 cells
| Mutant | Bmax | Kd (mutant/WT) | EC50 (mutant/WT) | Rmax | Q (mutant/WT) |
|---|---|---|---|---|---|
| % WT | % WT | ||||
| FSHR | |||||
| D153E (n = 2) | 90 ± 22 | 1.2 ± 0.4 | 1.5 ± 0.4 | 203 ± 1 | 1.8 ± 0.05 |
| D153N (n = 3) | 210 ± 51 | 3.2 ± 0.6 | 6.5 ± 1.8 | 130 ± 60 | 0.3 ± 0.06 |
| D153A (n = 4) | 49 ± 7 | 1.1 ± 0.2 | 25.0 ± 3.0 | 106 ± 9 | 0.5 ± 0.1 |
| D153K (n = 3) | 47 ± 1 | 0.6 ± 0.1 | >200 | ∼0 | a |
| LHR | |||||
| D157E (n = 5) | 234 ± 90 | 2.0 ± 0.5 | 2.4 ± 0.3 | 215 ± 76 | 1.1 ± 0.2 |
| D157N (n = 4) | 40 ± 8 | 3.9 ± 1.0 | >400 | a | a |
| D157A (n = 4) | 95 ± 35 | 13 ± 1 | >95 | a | a |
| D157K (n = 2) | 22 ± 8 | 2.4 ± 0.7 | a | ∼0 | a |
| TSHR | |||||
| D160E (n = 3) | b | c | 3.3 ± 0.5 | 56 ± 15 | c |
| D160N (n = 2) | b | c | 3.3 ± 1.2 | 56 ± 12 | c |
| D160A (n = 3) | b | c | 1.7 ± 0.1 | 68 ± 13 | c |
| D160K (n = 3) | b | c | 6.6 ± 0.4 | a | c |
a The EC50 was too high to permit accurate measurement of Rmax and Q.
b Data were not determined by binding (see Table 6).
c Data were not determined.