CYP2E1

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Cytochrome P450 2E1 (abbreviated CYP2E1, EC 1.14.14.1), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the body. While it is involved only in the oxidative metabolism of a small range of substrates (mostly small polar molecules), there are many important drug interactions mediated by CYP2E1.

CYP2E1 Ligands

Selected inducers, inhibitors and substrates of CYP2E1

Substrates	Inhibitors	Inducers
Often mentioned: anaesthetics halothane isoflurane enflurane paracetamol (analgesic, antipyretic) Other: dapsone (antibiotic) theophylline (stimulant) ethanol (psychoactive) chlorzoxazone (muscle relaxant) toluene (solvent) - primarily	Strong: diethyldithiocarbamate (in cancer) unspecified: cimetidine (H2-receptor antagonist) disulfiram (in alcoholism)	acetone (cleaning fluid) ethanol (psychoactive) isoniazid (in tuberculosis)

Regulation of CYP2E1

Within one day of birth, the rat hepatic CYP2E1 gene is activated transcriptionally. CYP2E1 expression is easily inducible. It seems that there exist two stages of induction, a posttranslational mechanism for increased protein stability at low levels of ethanol, and an additional transcriptional induction at high levels of ethanol

See also

• cytochrome
• metabolism

Further reading

• Smith G, Stubbins MJ, Harries LW, Wolf CR (1999). "Molecular genetics of the human cytochrome P450 monooxygenase superfamily". Xenobiotica. 28 (12): 1129–65. PMID 9890157.CS1 maint: Multiple names: authors list (link)
• Kessova I, Cederbaum AI (2003). "CYP2E1: biochemistry, toxicology, regulation and function in ethanol-induced liver injury". Curr. Mol. Med. 3 (6): 509–18. doi:10.2174/1566524033479609. PMID 14527082.