Atpenins, potent and specific inhibitors of mitochondrial complex II (succinate-ubiquinone oxidoreductase)
Atpenins, potent and specific inhibitors of mitochondrial complex II (succinate-ubiquinone oxidoreductase)
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DOI：
10.1073/pnas.0237315100
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发表时间：
2003-01-21
影响因子：
11.1
通讯作者：
Omura, S
中科院分区：
文献类型：
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作者：
Miyadera, H;Shiomi, K;Omura, S
线粒体呼吸链中的酶除了在通过氧化磷酸化产生ATP中起重要作用外，还参与各种生理事件。复合物I（NADH-泛醌还原酶）和复合物III（泛喹啉-细胞色素c还原酶）的特异性和有效的抑制剂（例如鱼藤酮和抗霉素）的使用分别允许确定这些酶在生理过程中的作用。然而，与复合物I、III和IV（细胞色素c氧化酶）不同，已经描述了复合物II（琥珀酸-泛醌还原酶）的很少有效和特异性抑制剂。在这篇文章中，我们报告atpenins有效地和特异性地抑制线粒体复合物III的琥珀酸泛醌还原酶活性。因此，atpenins可能是有用的工具，澄清的生化和结构特性的复合物II，以及确定其在哺乳动物组织中的生理作用。
Enzymes in the mitochondrial respiratory chain are involved in various physiological events in addition to their essential role in the production of ATP by oxidative phosphorylation. The use of specific and potent inhibitors of complex I (NADH-ubiquinone reductase) and complex III (ubiquinol-cytochrome c reductase), such as rotenone and antimycin, respectively, has allowed determination of the role of these enzymes in physiological processes. However, unlike complexes I, III, and IV (cytochrome c oxidase), there are few potent and specific inhibitors of complex II (succinate-ubiquinone reductase) that have been described. In this article, we report that atpenins potently and specifically inhibit the succinate-ubiquinone reductase activity of mitochondrial complex III. Therefore, atpenins may be useful tools for clarifying the biochemical and structural properties of complex II, as well as for determining its physiological roles in mammalian tissues.