What is the CYP2A6 gene?
What is the CYP2A6 gene?
Summary. This gene, CYP2A6, encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids.
What does CYP2A6 do?
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.
What does CYP2A6 metabolize?
CYP2A6, a phase I drug metabolizing enzyme (DME) which metabolizes about 3% of pharmaceutical agents including letrozole, tegafur, coumarin, valproic acid, methoxyflurane, artesunate, disulfiram, halothane and fadrozole.
What is a CYP2D6 substrate?
Cytochrome P450 2D6 (CYP2D6) is an enzyme that in humans is encoded by the CYP2D6 gene. CYP2D6 is primarily expressed in the liver. It is also highly expressed in areas of the central nervous system, including the substantia nigra.
What is cotinine found in?
Cotinine is an alkaloid found in tobacco leaves and the main metabolite of nicotine. The active form of cotinine, the isomer S(-)-cotinine accumulates in the body after tobacco consumption.
What is nicotine metabolized by?
Almost 90% of nicotine absorbed by the body is metabolized in the liver. Nicotine may also be metabolized in the kidneys, lungs, brain, and respiratory epithelium membranes. The nicotine undergoes many transformations. Key role in the metabolism of nicotine is played by cytochrome P450 oxidases (mainly CYP2A6).
What does CYP2D6 stand for?
CYP2D6 Gene – Cytochrome P450 Family 2 Subfamily D Member 6 This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids.
What are CYP2D6 drugs?
The CYP2D6 enzyme catalyses the metabolism of a large number of clinically important drugs including antidepressants, neuroleptics, some antiarrhythmics, lipophilic β-adrenoceptor blockers and opioids.
What is the importance of CYP3A4?
Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14. 13.97) is an important enzyme in the body, mainly found in the liver and in the intestine. It oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from the body.
What cotinine means?
Listen to pronunciation. (KOH-tuh-neen) A chemical substance formed by the breakdown of nicotine in the body. Nicotine is an addictive, harmful chemical found in tobacco and tobacco products, including cigarettes and chewing tobacco.
What is the difference between nicotine and cotinine?
Cotinine is a product formed after the chemical nicotine enters the body. Nicotine is a chemical found in tobacco products, including cigarettes and chewing tobacco.
What is the chemical formula for nicotine?
C₁₀H₁₄N₂Nicotine / Formula
What is the name of the enzyme that metabolizes nicotine?
Nicotine is metabolized primarily by the liver enzymes CYP2A6, UDP-glucuronosyltransfease (UGT), and flavin-containing monooxygenase (FMO).
What is metabolized by 2d6?
What is a drug metabolized by CYP2D6?
Multiple tricyclic antidepressants, β blockers, haloperidol, sertraline, paroxetine, and thioridazine are among the common drugs metabolized by CYP2D6.
Why is CYP2D6 important?
CYP2D6 is responsible for the metabolism of the second highest number of drugs metabolized by P450 enzymes. Substrates for CYP2D6 can be found in Table 3.1. CYP2D6 is a particularly challenging enzyme to understand and study because of its genetic polymorphism.
What are CYP3A4 drugs?
Potent inhibitors of CYP3A4 include clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, goldenseal and grapefruit. Inducers of CYP3A4 include phenobarbital, phenytoin, rifampicin, St. John’s Wort and glucocorticoids.
What does it mean if a drug is metabolized by CYP3A4?
The human CYP2A gene subfamily consists of three members, CYP2A6, CYP2A7, and CYP2A13. The CYP2A6 gene is highly polymorphic with approximately 40 annotated allelic variants. Individuals homozygous for some of these alleles have a total lack of CYP2A6 activity.
What is cytochrome P450 2A6 used for?
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.
Is CYP2A6 genetic polymorphism a risk factor for tobacco-related cancer?
Kamataki T, Fujieda M, Kiyotani K, et al. (2005). “Genetic polymorphism of CYP2A6 as one of the potential determinants of tobacco-related cancer risk”. Biochem. Biophys. Res. Commun. 338 (1): 306–10. doi: 10.1016/j.bbrc.2005.08.268. PMID 16176798.
What causes interindividual variability in CYP2A6 apoprotein levels?
Significant interindividual variability in CYP2A6 apoprotein and mRNA levels has been observed. CYP2A6 is known to be inducible by phenobarbital and rifampicin, and it is suspected that other antiepileptic drugs may also have this effect.