Haloenol lactones as inactivators and substrates of aldehyde dehydrogenase

• Published in: Journal of protein chemistry Vol. 15; no. 7; p. 639
• Main Authors: Mukerjee, N, Dryjanski, M, Dai, W, Katzenellenbogen, J A, Pietruszko, R
• Format: Journal Article
• Language: English
• Published: United States 01.10.1996
• Subjects: Aldehyde Dehydrogenase - antagonists & inhibitors; Aldehyde Dehydrogenase - metabolism; Binding Sites; Chromatography, High Pressure Liquid; Cysteine - metabolism; Enzyme Inhibitors - pharmacology; Esterases - metabolism; Humans; Hydrolysis; Isoenzymes - metabolism; Kinetics; Lactones - metabolism; Lactones - pharmacology; Molecular Structure; Pyrones - metabolism; Pyrones - pharmacology; Substrate Specificity

Human aldehyde dehydrogenase (EC 1.2.1.3) isozymes E1 and E2 were irreversibly inactivated by stoichiometric concentrations of the haloenol lactones 3-isopropyl-6(E)-bromomethylene tetrahydro-pyran-2-one and 3-phenyl-6(E)-bromomethylene tetrahydropyran-2-one. No inactivation occurred with the corres...