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某些吡啶衍生物对心脏NAD糖水解酶活性的影响

[Effect on some pyridine derivatives on the activity of heart NAD glycohydrolase].

作者信息

Prikhod'ko A Z, Boriskina G M, Mal'tsev N I

出版信息

Biokhimiia. 1977 Jul;42(7):1232-6.

PMID:198025
Abstract

Effect of some 3- and 4-substituted pyridines on enzymatic hydrolysis of NAD by rabbit heart muscle NAD-glycohydrolase has been studied. It is shown that some 4-substituted derivatives in contrast with 3-substituted ones produce an inhibitory effect on the enzyme activity. A new efficient inhibitor of rabbit heart muscle NAD-glycohydrolase (I50 = 10(-3) M)--N1-(2-lactyl)-N2-(isonicotinoy)hydrazine, inducing uncompetitive inhibition of hydrolysis of NAD is found. The mechanism of the inhibitory effect of N1-(2-lactyl)-N2-(isonicotinoyl)hydrazine was investigated and the rate equation for enzymatic hydrolysis of NAD in the presence of inhibitor is calculated. It is suggested, that the inhibitory effect of N1-(2-lactyl)-N2-(isonicotinoyl)hydrazine is due to the formation of triple inactive complex inhibitor-enzyme-adenosinediphosphateribose.

摘要

研究了某些3-和4-取代吡啶对兔心肌NAD-糖水解酶催化NAD酶促水解的影响。结果表明,与3-取代衍生物相比,某些4-取代衍生物对酶活性产生抑制作用。发现了一种新的高效兔心肌NAD-糖水解酶抑制剂(I50 = 10^(-3) M)——N1-(2-乳酰基)-N2-(异烟酰基)肼,它对NAD水解产生非竞争性抑制。研究了N1-(2-乳酰基)-N2-(异烟酰基)肼的抑制作用机制,并计算了存在抑制剂时NAD酶促水解的速率方程。有人提出,N1-(2-乳酰基)-N2-(异烟酰基)肼的抑制作用是由于形成了抑制剂-酶-腺苷二磷酸核糖的三元无活性复合物。

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