Table 3. Relative Binding Affinities of Ligands to the Wild-Type C1b Domain of PKCδ and to Mutated Versions Incorporating One or More of the Residues of PKCζ/ι Responsible for Its Loss of Ligand Binding Activity.
Kd or Ki relative
to that for PDBu binding to the wtδC1ba |
|||||||||
---|---|---|---|---|---|---|---|---|---|
compd | Kd, nM,a wtδC1B | N7R | S10R | P11R | L20R | N7R/P11R | N7R/L20R | N7R/S10R/P11R | N7R/S10R/L20R |
PDBu | (0.23) | 5.13 | 1.39 | 5.17 | 34.7 | 147 | 2090 | 85.2 | 5900 |
1-E | (2.95) | 1.12 | 0.79 | 3.53 | 4.75 | 12.5 | 81.0 | 21.3 | 224 |
2-E | (2.46) | 1.01 | 0.85 | 0.94 | 7.87 | NTb | NTb | NTb | NTb |
3-E | (2.95) | 0.67 | 0.40 | 0.50 | 3.20 | NTb | NTb | NTb | NTb |
4-E | (2102) | 0.30 | 0.40 | 0.20 | 1.34 | 2.47 | 21.8 | NTb | NTb |
5-E | (560) | 1.41 | 1.45 | 1.27 | 12.4 | 6.79 | 209 | NTb | NTb |
5-Z | (865) | 0.55 | 0.57 | 1.09 | 3.25 | 3.25 | 60.0 | NTb | NTb |
6-E | (1206) | 1.44 | 1.46 | 2.79 | 4.57 | 13.2 | 87.0 | NTb | NTb |
7-E | (1070) | 0.82 | 0.62 | 0.93 | 5.74 | 3.49 | 78.0 | NTb | NTb |
8-E | (300) | 0.94 | 1.56 | 0.33 | 5.33 | NTb | NTb | NTb | NTb |
9-E | (96) | 1.25 | 0.98 | 1.25 | 7.70 | NTb | NTb | NTb | NTb |
10-E | (1) | 0.90 | 1.50 | 1.70 | 17.3 | NTb | NTb | NTb | NTb |
11-E | (0.5) | 1.20 | 1.20 | 2.00 | 17.6 | NTb | NTb | NTb | NTb |
12-E | (0.6) | 1.17 | 1.00 | 2.00 | 17.5 | NTb | NTb | NTb | NTb |
13-E | (777) | 1.04 | 1.44 | 2.61 | 1.04 | 30.7 | 9.83 | 60.5 | 10.1 |
Data are derived from Table 2.
NT, not tested.