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Licensed Unlicensed Requires Authentication Published by De Gruyter May 5, 2012

CYP2A6: genetics, structure, regulation, and function

  • Hannu Raunio EMAIL logo and Minna Rahnasto-Rilla

Abstract

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. The CYP2A6 protein is most abundant in liver and is expressed, although at much lower levels, in some other tissues, especially nasal mucosa. CYP2A6 differs from other human liver CYP forms in that it participates in the metabolism of very few currently used drugs. The two most relevant substrates for CYP2A6 are coumarin and nicotine. Coumarin is the marker substance for determining CYP2A6 activity both in vitro and in vivo. Approximately 80% of a nicotine dose is eliminated by CYP2A6, and there is a clear link between CYP2A6 genotypes, smoking behavior, and lung cancer risk.


Corresponding authors: Hannu Raunio and Minna Rahnasto-Rilla, Faculty of Health Sciences, School of Pharmacy, University of Eastern Finland, Box 1627, 70211 Kuopio, Finland

Received: 2012-1-18
Accepted: 2012-2-24
Published Online: 2012-05-05
Published in Print: 2012-06-01

©2012 by Walter de Gruyter Berlin Boston

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