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羟基柠檬酸异构体对柠檬酸合酶、柠檬酸裂解酶和ATP柠檬酸裂解酶的反应活性及抑制潜力

Reactivity and inhibitor potential of hydroxycitrate isomers with citrate synthase, citrate lyase, and ATP citrate lyase.

作者信息

Sullivan A C, Singh M, Srere P A, Glusker J P

出版信息

J Biol Chem. 1977 Nov 10;252(21):7583-90.

PMID:334761
Abstract

The four isomers of hydroxycitrate have been tested as substrates and inhibitors for citrate synthase, citrate lyase, and ATP citrate lyase. None of the isomers served as a substrate for citrate synthase and they were moderate to weak inhibitors of this reaction. Of the four isomers, only (pncit)-(2S)-2-hydroxycitrate did not serve as a substrate for citrate lyase while (pncit)-(4S)-4-hydroxycitrate was the only isomer which did not serve as a substrate for ATP citrate lyase. No consistent pattern of reactivity or inhibitor potency was seen with the different isomeric hydroxycitrates. It is proposed that more than one mode of binding is possible between the isomers and the three different active sites.

摘要

羟基柠檬酸的四种异构体已作为柠檬酸合酶、柠檬酸裂解酶和ATP柠檬酸裂解酶的底物及抑制剂进行了测试。这些异构体均不能作为柠檬酸合酶的底物,且对该反应为中度至弱抑制剂。在这四种异构体中,只有(pncit)-(2S)-2-羟基柠檬酸不能作为柠檬酸裂解酶的底物,而(pncit)-(4S)-4-羟基柠檬酸是唯一不能作为ATP柠檬酸裂解酶底物的异构体。不同的异构羟基柠檬酸未呈现出一致的反应模式或抑制效力。有人提出,异构体与三种不同活性位点之间可能存在不止一种结合模式。

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Reactivity and inhibitor potential of hydroxycitrate isomers with citrate synthase, citrate lyase, and ATP citrate lyase.羟基柠檬酸异构体对柠檬酸合酶、柠檬酸裂解酶和ATP柠檬酸裂解酶的反应活性及抑制潜力
J Biol Chem. 1977 Nov 10;252(21):7583-90.
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