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Table 2 (Abstract A19). Affinity and activation constants measurements of PKG I and II for cGMP and analogs

From: Abstracts from the 8th International Conference on cGMP Generators, Effectors and Therapeutic Implications

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)
  1. Footnote:
  2. EC50 and K A values were measured using competitive surface plasmon resonance and microfluidic mobility shift assay. (n) = Number of measurements.