Inhibition of renal gluconeogenesis and phosphoenolpyruvate carboxykinase activity by 3-mercaptopicolinic acid: studies in rat, guinea pig, dog, rabbit, and man.
Inhibition of renal gluconeogenesis and phosphoenolpyruvate carboxykinase activity by 3-mercaptopicolinic acid: studies in rat, guinea pig, dog, rabbit, and man.
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3-巯基甲酸抑制肾糖异生和磷酸烯醇丙酮酸羧激酶活性：在大鼠、豚鼠、狗、兔和人中的研究。
DOI：
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发表时间：
1980
期刊：
影响因子：
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通讯作者：
A. Gougoux
中科院分区：
文献类型：
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作者：
M. Watford;P. Vinay;G. Lemieux;A. Gougoux
3-巯基吡啶甲酸酯（磷酸烯醇丙酮酸羧激酶反应的特异性抑制剂）对离体肾小管上皮细胞增生的抑制具有种属特异性。在任何给定的抑制剂浓度下，抑制程度的顺序为大鼠>豚鼠大于或等于人>兔大于或等于狗。PEPCK活性的细胞内分布（如在前向和后向方向上测量的）支持以下结论：在完整细胞中，胞质酶优先被抑制。抑制分析未能证明酶之间的任何显著差异，无论细胞内或动物来源。当正向测定时，所有酶对3-巯基吡啶甲酸酯显示相似的Ki（2- 10 μ M）。观察到的优先胞浆抑制可能是由于金属离子浓度的原位差异或线粒体对巯基吡啶甲酸盐渗透性的限制。
The inhibition of gluconeogenesis in isolated kidney tubules by 3-mercaptopicolinate, a specific inhibitor of the phosphoenolpyruvate carboxykinase reaction, is species specific. At any given concentration of the inhibitor, the degree of inhibition is in the order rat > guinea pig greater than or equal to man > rabbit greater than or equal to dog. The intracellular distribution of PEPCK activity (as measured in both the forward and backward directions) supports the conclusion that in the intact cell the cytosolic enzyme is preferentially inhibited. Analysis of the inhibition failed to demonstrate any significant differences between the enzymes, regardless of intracellular or animal source. All enzymes exhibited a similar Ki (2--10 microM) for 3-mercaptopicolinate when assayed in the forward direction. The observed preferential cytosolic inhibition could be due to either in situ differences in metallic ions concentration or a restriction in mitochondrial permeability for mercaptopicolinate.