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Drug Metabolism and Personalized Therapy

Official journal of the European Society of Pharmacogenomics and Personalised Therapy

Editor-in-Chief: Llerena, Adrián

Editorial Board Member: Chen, Bing / Dahl, Marja-Liisa / Devinsky, Ferdinand / Hirata, Rosario / Hubacek, Jaroslav A. / Ingelman-Sundberg, Magnus / Maitland-van der Zee, Anke-Hilse / Manolopoulos, Vangelis G. / Marc, Janja / Melichar, Bohuslav / Meyer, Urs A. / Nair, Sujit / Nofziger, Charity / Peiro, Ana / Sadee, Wolfgang / Salazar, Luis A. / Simmaco, Maurizio / Turpeinen, Miia / Schaik, Ron / Shin, Jae-Gook / Visvikis-Siest, Sophie / Zanger, Ulrich M.

4 Issues per year


CiteScore 2016: 1.40

SCImago Journal Rank (SJR) 2016: 0.413
Source Normalized Impact per Paper (SNIP) 2016: 0.537

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2363-8915
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Volume 27, Issue 2 (Jun 2012)

Issues

CYP2A6: genetics, structure, regulation, and function

Hannu Raunio
  • Corresponding author
  • Faculty of Health Sciences, School of Pharmacy, University of Eastern Finland, Kuopio, Finland
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  • Other articles by this author:
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/ Minna Rahnasto-Rilla
  • Corresponding author
  • Faculty of Health Sciences, School of Pharmacy, University of Eastern Finland, Kuopio, Finland
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
Published Online: 2012-05-05 | DOI: https://doi.org/10.1515/dmdi-2012-0001

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.

Keywords: cigarette smoking; CYP2A6; genetic polymorphisms; nicotine

About the article

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: 2012-01-18

Accepted: 2012-02-24

Published Online: 2012-05-05

Published in Print: 2012-06-01


Citation Information: , ISSN (Online) 2191-0162, ISSN (Print) 0792-5077, DOI: https://doi.org/10.1515/dmdi-2012-0001.

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©2012 by Walter de Gruyter Berlin Boston. Copyright Clearance Center

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