Pharmacogenetics of membrane transporters: A review of current approaches

Tristan M. Sissung, Erin R. Gardner, Rui Gao, William D. Figg

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

22 Scopus citations


This chapter provides a review of the pharmacogenetics of mem brane transporters, including adenosine triphosphate-binding cassette (ABC) transporters and organic anion transporting proteins (OATPs). Membrane trans porters are heavily involved in drug disposition by actively transporting substrate drugs between organs and tissues. As such, polymorphisms in the genes encoding these proteins may have a significant effect on the absorption, distribution, metabo lism, and excretion of compounds. The techniques used to identify substrates and inhibitors of these proteins and subsequently assess the effect of genetic mutation on transport, both in vitro and in vivo, are outlined and discussed. Finally, studies linking transporter genotype with clinical outcomes are discussed.

Original languageEnglish
Title of host publicationPharmacogenomics in Drug Discovery and Development
Subtitle of host publicationFrom Bench to Bedside
PublisherHumana Press
Number of pages22
ISBN (Print)9781588298874
StatePublished - 2008

Publication series

NameMethods in Molecular Biology
ISSN (Print)1064-3745


  • ABCB1
  • ABCC1
  • ABCC2
  • ABCG2
  • OATP1B1
  • OATP1B3
  • Polymor phisms
  • Transport


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