The Effect of Nitroxyalkyl Succinimides on Activity of Cyclic Guanosine Monophosphate Phosphodiesterase

被引：0
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作者：
L. V. Tat’yanenko
O. V. Dobrokhotova
M. A. Fadeev
A. B. Eremeev
A. N. Utyonishev
V. V. Tkachev
N. S. Goryachev
A. I. Kotelnikov
B. S. Fedorov
机构：
[1] Russian Academy of Sciences,Institute of Problems of Chemical Physics
[2] M. V. Lomonosov Moscow State University,undefined
来源：
Bulletin of Experimental Biology and Medicine | 2020年 / 168卷
关键词：
cGMP phosphodiesterase; N-nitroxyalkyl succinimides; inhibition; X-ray analysis;
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摘要：
The effect of N-nitroxymethyl succinimide (1), N-(2-nitroxyethyl) succinimide (2) and N-(3-nitroxypropyl) succinimide (3) on enzymatic activity of cyclic guanosine monophosphate (cGMP) phosphodiesterase was studied and crystal structure of compound (2) was determined. It was shown that all studied N-nitroxy succinimides inhibited cGMP phosphodiesterase in a concentration range of 0.1-0.001 mM. Compound (2) noncompetitively and reversibly inhibited hydrolytic function of enzyme with Ki=1.7×10—5 М. Inhibition constant for the reference compound N-(2-nitroethyl) nicotinamide (nicorandil) was 3×10—5 М.
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页码：330 / 333
页数：3
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