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[羧酸阴离子(底物类似物)对乳酸脱氢酶的非线性、非竞争性抑制作用]

[Non-linear, non-competitive inhibition of lactate dehydrogenase with carboxylic acid anions (substrate analogues)].

作者信息

Saburova E A, Gol'dshteĭn B N, Elfimova L I, Vol'kenshteĭn M V

出版信息

Mol Biol (Mosk). 1982 Nov-Dec;16(6):1173-82.

PMID:7155138
Abstract

The carboxylic acid anions are shown to inhibit lactate dehydrogenase in a non-competitive manner at pH 8.5. The inhibitory effect of different carboxylates used increases in the direction acetate leads to formate leads to methacrylate. Non-competitive inhibition by carboxylates has a non-linear character with effective Hill exponent depending on the inhibitor concentration increasing to the value n approximately equal to 2 when inhibitor concentration increases. The kinetic model is proposed to account for non-linear non-competitive inhibition in consequence of the abortive ternary complexes formation in two enzyme conformations. The substrate analogues properties that result in non-competitive inhibition of lactatedehydrogenase are considered.

摘要

研究表明,羧酸根阴离子在pH 8.5时以非竞争性方式抑制乳酸脱氢酶。所使用的不同羧酸盐的抑制作用按乙酸盐→甲酸盐→甲基丙烯酸盐的顺序增强。羧酸盐的非竞争性抑制具有非线性特征,有效希尔系数取决于抑制剂浓度,当抑制剂浓度增加时,该系数增加至约等于2的值n。提出了动力学模型来解释由于两种酶构象中形成无效三元复合物而导致的非线性非竞争性抑制。考虑了导致乳酸脱氢酶非竞争性抑制的底物类似物特性。

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