Table 2 (Abstract A19). Affinity and activation constants measurements of PKG I and II for cGMP and analogs
| Affinity Measurements of PKG I and II Regulatory Dimers | ||||
| PKG Iβ | ||||
|
hPKG Iβ 1-351 | cGMP | 8-Br-cGMP | 8-pCPT-cGMP | PET-cGMP |
| WT |
163±6 nM (2) |
222±4 nM (2) |
212±20 nM (3) |
3.8±0.4 nM (2) |
| G182E |
328±6 nM (2) |
765±25 nM (2) |
206±18 nM (2) |
5.8±0.4 nM (2) |
| G306E |
4.2±0.1 nM (3) |
< 2 nM (2) |
7.7±0.4 nM (2) |
<< 2 nM (2) |
| PKG II | ||||
|
hPKG II 41-418 | cGMP | 8-Br-cGMP | 8-pCPT-cGMP | PET-cGMP |
| WT |
96±5 nM (3) |
20±2 nM (3) |
5±1 nM (3) |
193±10 nM (3) |
| G232E |
184±0.1 nM (2) |
11±1 nM (2) |
116±8 nM (2) |
1963±12 nM (2) |
| G356E |
50±3 nM (3) |
30±2 nM (2) |
≤ 1.1±0.3 nM (2) |
5.3±0.3 nM (2) |
| Activation Constant Measurements of PKG I and II Full Lengths | ||||
| cGMP | 8-Br-cGMP | 8-pCPT-cGMP | PET-cGMP | |
|
hPKG Iβ 5-678 |
370±13 nM (4) |
206±13 nM (3) |
249±17 nM (3) |
18±2 nM (3) |
|
hPKG II 40-762 |
257±11 nM (3) |
58±5 nM (3) |
22±3 nM (4) |
225±13 nM (3) |
