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3-巯基吡啶甲酸对嗜热四膜虫中磷酸烯醇式丙酮酸羧激酶及糖异生的抑制作用。

Inhibition of P-enolpyruvate carboxykinase and of glyconeogenesis in Tetrahymena by 3-mercaptopicolinic acid.

作者信息

Liang T, Raugi G J, Blum J J

出版信息

J Protozool. 1976 Aug;23(3):473-7. doi: 10.1111/j.1550-7408.1976.tb03816.x.

Abstract

Tetrahymena grown overnight in deep cultures were incubated for 1 hr with [1-14C]labeled substrates in the presence or absence of 3-mercaptopicolinic acid (3MPA). 3-MPA inhibited appearance of label in glycogen from bicarbonate, acetate, pentanoate, octanoate, and succinate, but not from glycerol or glucose. In vitro assays of phosphoenolpyruvate carboxylase and phosphoenolpyruvate carboxykinase activity showed that both enzymes were about equally distributed between the particulate and cytosol fractions. 3-MPA inhibited phosphoenolpyruvate carboxykinase from both the cytoplasmic and particulate fractions, but had no effect on phosphoenolpyruvate carboxylase from either location. These results suggest that the in vivo effects of this drug are due to inhibition of glyconeogenesis at this site.

摘要

在深层培养中过夜培养的四膜虫,在存在或不存在3-巯基吡啶甲酸(3MPA)的情况下,与[1-¹⁴C]标记的底物孵育1小时。3MPA抑制了来自碳酸氢盐、乙酸盐、戊酸盐、辛酸盐和琥珀酸盐的糖原中标记物的出现,但不抑制来自甘油或葡萄糖的糖原中标记物的出现。磷酸烯醇式丙酮酸羧化酶和磷酸烯醇式丙酮酸羧激酶活性的体外测定表明,这两种酶在颗粒部分和胞质溶胶部分中的分布大致相等。3MPA抑制了细胞质和颗粒部分的磷酸烯醇式丙酮酸羧激酶,但对这两个位置的磷酸烯醇式丙酮酸羧化酶均无影响。这些结果表明,该药物的体内作用是由于在此位点抑制糖异生作用。

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