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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.