Greenhut J, Umezawa H, Rudolph F B
J Biol Chem. 1985 Jun 10;260(11):6684-6.
S-2,3-Dicarboxyaziridine was found to be a potent competitive inhibitor (Ki = 0.08 microM) of fumarase from pig heart. The aziridine did not inactivate the enzyme or exhibit any observable substrate activity. It is likely that it functions as a transition state analogue mimicking the carbanion intermediate found in the normal catalytic reaction. The aziridine inhibited fumarate utilization in ruptured but not intact mitochondria.
已发现S-2,3-二羧基氮丙啶是猪心延胡索酸酶的一种有效竞争性抑制剂（Ki = 0.08微摩尔）。该氮丙啶不会使酶失活，也没有表现出任何可观察到的底物活性。它可能作为一种过渡态类似物，模拟正常催化反应中发现的碳负离子中间体。该氮丙啶抑制破裂线粒体中延胡索酸的利用，但不抑制完整线粒体中延胡索酸的利用。
