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[生物活性化合物的有机磷酸类似物。十四。作为乙酰辅酶A羧化酶抑制剂的ATP的卤代膦酸酯类似物]

[Organophosphate analogs of biologically active compounds. XIV. Halophosphonate analogs of ATP as acetyl CoA carboxylase inhibitors].

作者信息

Biriukov A I, Tarusova N B, Amontov S G, Osipova T I, Goriachenkova E V

出版信息

Bioorg Khim. 1985 May;11(5):598-604.

PMID:2864043
Abstract

Halophosphonate ATP analogues pp[CHBr]pA and p[CHBr]ppA synthesised from bromomethylenebisphosphonate and adenosine derivatives, proved to be effective competitive inhibitors of Ac-CoA-carboxylase (CE 6.4.1.2) from rat liver (Ki = 0,2 mM). The inhibitory effects of both analogues were reversible and higher than those of some other ATP analogues. Another enzyme, Ac-CoA-synthetase (CE 6.2.1.1), with a different mode of ATP-cleavage showed wider specificity to ATP-analogues than Ac-CoA-carboxylase.

摘要

由溴亚甲基双膦酸酯和腺苷衍生物合成的卤代膦酸酯ATP类似物pp[CHBr]pA和p[CHBr]ppA,被证明是大鼠肝脏中乙酰辅酶A羧化酶(EC 6.4.1.2)的有效竞争性抑制剂(Ki = 0.2 mM)。这两种类似物的抑制作用都是可逆的,且比其他一些ATP类似物的抑制作用更强。另一种酶,乙酰辅酶A合成酶(EC 6.2.1.1),具有不同的ATP裂解模式,与乙酰辅酶A羧化酶相比,对ATP类似物表现出更广泛的特异性。

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