Inhibition of fumarase by S-2,3-dicarboxyaziridine.
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.
D001388:Aziridines / Q000494:pharmacology*; D001389:Azirines / Q000494:pharmacology*; D005649:Fumarate Hydratase / Q000037:antagonists & inhibitors*; D007700:Kinetics; D008930:Mitochondria, Liver / Q000187:drug effects / Q000378:metabolism; D010101:Oxygen Consumption / Q000187:drug effects
D001388:Aziridines; D001389:Azirines; C045613:2,3-dicarboxyaziridine; D005649:Fumarate Hydratase