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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.
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