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) |