串珠镰刀菌素对丙酮酸脱氢酶复合体的抑制作用。
Inhibition of pyruvate dehydrogenase complex by moniliformin.
作者信息
Gathercole P S, Thiel P G, Hofmeyr J H
出版信息
Biochem J. 1986 Feb 1;233(3):719-23. doi: 10.1042/bj2330719.
Abstract
The mechanism for the inhibition of pyruvate dehydrogenase complex from bovine heart by moniliformin was investigated. Thiamin pyrophosphate proved to be necessary for the inhibitory action of moniliformin. The inhibition reaction was shown to be time-dependent and to follow first-order and saturation kinetics. Pyruvate protected the pyruvate dehydrogenase complex against moniliformin inactivation. Extensive dialysis of the moniliformin-inactivated complex only partially reversed inactivation. Moniliformin seems to act by inhibition of the pyruvate dehydrogenase component of the enzyme complex and not by acting on the dihydrolipoamide transacetylase or dehydrogenase components, as shown by monitoring the effect of moniliformin on each component individually. On the basis of these results, a suicide inactivator mechanism for moniliformin on pyruvate dehydrogenase is proposed.
摘要
研究了新月霉素对牛心丙酮酸脱氢酶复合体的抑制机制。事实证明，硫胺素焦磷酸对于新月霉素的抑制作用是必需的。抑制反应表现出时间依赖性，并符合一级动力学和饱和动力学。丙酮酸可保护丙酮酸脱氢酶复合体免受新月霉素的失活作用。对被新月霉素失活的复合体进行广泛透析只能部分逆转失活。如通过分别监测新月霉素对每个组分的作用所示，新月霉素似乎是通过抑制酶复合体中的丙酮酸脱氢酶组分起作用，而不是作用于二氢硫辛酰胺转乙酰酶或脱氢酶组分。基于这些结果，提出了新月霉素对丙酮酸脱氢酶的自杀性失活机制。
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