Cytochrome P450 2A6 (abbreviated CYP2A6) is a member of the cytochrome P450 mixed-function oxidase system, which is involved in the metabolism of xenobiotics in the body. CYP2A6 is the primary enzyme responsible for the oxidation of nicotine and cotinine. It is also involved in the metabolism of several pharmaceuticals, carcinogens, and a number of coumarin-type alkaloids. CYP2A6 is the only enzyme in the human body that appreciably catalyzes the 7-hydroxylation of coumarin, such that the formation of the product of this reaction, 7-hydroxycoumarin, is used as a probe for CYP2A6 activity. Cytochrome P450 Oxidase (CYP2E1) Cytochrome P450 oxidase (commonly abbreviated CYP) is a generic term for a large number of related, but distinct, oxidative enzymes (EC 1. ... A xenobiotic is a chemical which is found in an organism but which is not normally produced or expected to be present in it. ... Nicotine is an organic compound, an alkaloid found naturally throughout the tobacco plant, with a high concentration in the leaves. ... Cotinine is a break-down product of nicotine from cigarette smoke. ... Coumarin is a chemical compound. ...

Distribution

CYP2A6 is found predominately in the liver.

Variability

Significant interindividual variability in CYP2A6 apoprotein and mRNA levels has been observed.

Induction

CYP2A6 is known to be inducible by phenobarbital and rifampicin, and it is suspected that other antiepileptic drugs may also have this effect. Phenobarbital (also phenobarbitone or luminal) is a weak acid with the chemical formula C12H12N2O3. ... Rifampicin (INN) or rifampin (USAN) is a bacteriocidal (kills bacteria) rather than bacteriostatic (keeps bacteria from replicating) antibiotic drug of the rifamycin group. ...

CYP2A6 Ligands

Phenobarbital (also phenobarbitone or luminal) is a weak acid with the chemical formula C12H12N2O3. ... Rifampicin (INN) or rifampin (USAN) is a bacteriocidal (kills bacteria) rather than bacteriostatic (keeps bacteria from replicating) antibiotic drug of the rifamycin group. ... Binomial name Citrus × paradisi Macfad. ... Flavonoids are a group of chemical compounds naturally found in certain fruits, vegetables, teas, wines, nuts, seeds, and roots. ... Ketoconazole is a synthetic antifungal drug used to prevent and treat skin and fungal infections, especially in immunocompromised patients such as those with AIDS. Due to its side-effect profile, it has been superseded by newer antifungals, such as Fluconazole and Itraconazole. ... Pilocarpine is a muscarinic alkaloid obtained from the leaves of tropical American shrubs from the genus Pilocarpus. ... Tranylcypromine is an antidepressant drug. ... Chemical structure of Aflatoxin B1 Aflatoxins are naturally occurring mycotoxins that are produced by many species of Aspergillus; but most notably Aspergillus flavus and Aspergillus parasiticus. ... Butadiene can refer to either one of two hydrocarbon chemical compounds which are alkenes that are isomers of each other. ... Cotinine is a break-down product of nicotine from cigarette smoke. ... Coumarin is a chemical compound. ... Structural formula of halothane Halothane vapour is an inhalational general anaesthetic. ... MTBE is highly flammable and is widely used as an oxygenate. ... Nicotine is an organic compound, an alkaloid found naturally throughout the tobacco plant, with a high concentration in the leaves. ... Quinoline, also known as 1-azanaphthalene, 1-benzazine, or benzo[b]pyridine, is a heterocyclic aromatic organic compound. ... Valproic acid or 2-Propylpentanoic acid is CH3CH2CH2CH(CH2CH2CH3)COOH . ...

References

• Pelkonen O, Rautio A, Raunio H, Pasanen M (2000). CYP2A6: a human coumarin 7-hydroxylase. Toxicology 144, 139–147.