Pharmacogenetics of Membrane Transporters

A Review of Current Approaches
  • Tristan M. Sissung
  • Erin R. Gardner
  • Rui Gao
  • William D. Figg
Part of the Methods in Molecular Biology™ book series (MIMB, volume 448)


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.


ABCB1 ABCC1 ABCC2 ABCG2 OATP1B1 OATP1B3 polymor phisms transport 


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Copyright information

© Humana Press, a part of Springer Science+Business Media, LLC 2008

Authors and Affiliations

  • Tristan M. Sissung
    • 1
  • Erin R. Gardner
    • 2
  • Rui Gao
    • 1
  • William D. Figg
    • 1
  1. 1.Clinical Pharmacology Program, Medical Oncology Branch, Center for Cancer ResearchNational Cancer InstituteBethesdaMaryland
  2. 2.Clinical Pharmacology ProgramSAIC-Frederick Inc.NCI-FrederickMaryland

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