Mechanism-Based Inactivation of Cytochromes P450 2E1 and 2E1 T303A by tert-Butyl Acetylenes: Characterization of Reactive Intermediate Adducts to the Heme and Apoprotein

The kinetics for the inactivation of cytochrome P450 2E1 and the mutant P450 2E1 T303A by tert-butyl acetylene (tBA) and tert-butyl 1-methyl-2-propynyl ether (tBMP) were investigated. The two acetylenes inactivated the 7-ethoxy-4-(trifluoromethyl)coumarin (7-EFC) O-deethylation activity of purified...

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Veröffentlicht in:	Chemical research in toxicology 2002-12, Vol.15 (12), p.1561-1571
Hauptverfasser:	Blobaum, Anna L, Kent, Ute M, Alworth, William L, Hollenberg, Paul F
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylene - analogs & derivatives Acetylene - pharmacology Alkylation - drug effects Amino Acid Substitution Animals Apoproteins - analysis Apoproteins - chemistry Carbon Monoxide - chemistry Chromatography, High Pressure Liquid - methods CYP2E1 protein Cytochrome P-450 CYP2E1 - chemistry Cytochrome P-450 CYP2E1 - genetics Cytochrome P-450 CYP2E1 Inhibitors Dose-Response Relationship, Drug Enzyme Activation Enzyme Inhibitors - pharmacology Heme - analysis Heme - chemistry Hydroxylation - drug effects Kinetics NADP - metabolism NADP - pharmacology Rabbits Recombinant Proteins - antagonists & inhibitors Recombinant Proteins - chemistry Recombinant Proteins - genetics Spectrometry, Mass, Electrospray Ionization Spectrophotometry, Ultraviolet Substrate Specificity tert-butyl 1-methyl-2-propynyl ether
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