Table 2. Binding of PDBu and DOG to PKCθC1B domain variants.
WT, wild-type.
| PKCθ C1B WT | PKCθ C1B Y239A | PKCθ C1B T243A | PKCθ C1B W253G | PKCθ C1B L255G | PKCθ C1B Q258G | |
|---|---|---|---|---|---|---|
| PDBu Kd (nM)* | 0.39 ± 0.2 | 3.32 ± 0.34 | 0.64 ± 0.06 | 2.95 ± 0.19 | 4.44 ± 0.56 | 670 ± 150 |
| DOG Ki (nM)* | 16.1 ± 0.7 | 86 ± 15 | 21.5 ± 1.8 | 470 ± 69 | 76 ± 24 | 1840 ± 320 |
| Ki/Kd | 41 | 26 | 34 | 159 | 17 | 3 |
| SAG Ki (nM)* | 8.7 ± 2.0 | 35.1 ± 5.1 | 5.5 ± 1.5 | 271 ± 22 | 71 ± 10 | 2260 ± 330 |
| Ki/Kd | 22 | 11 | 9 | 92 | 16 | 3 |
Values represent the means ± S.E.M. of triplicate independent experiments.