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Pharmacogenetics of Membrane Transporters: An Update on Current Approaches

  1. Author:
    Sissung, T. M.
    Baum, C. E.
    Kirkl, C. T.
    Gao, R.
    Gardner, E. R.
    Figg, W. D.

  2. Author Address

    [Baum, Caitlin E.; Kirkland, C. Tyler; Gao, Rui; Figg, William D.] NCI, Mol Pharmacol Sect, Med Oncol Branch, Ctr Canc Res, Bethesda, MD 20892 USA. [Sissung, Tristan M.; Figg, William D.] NCI, Clin Pharmacol Program, Med Oncol Branch, Ctr Canc Res, Bethesda, MD 20892 USA. [Gardner, Erin R.] NCI, Clin Pharmacol Program, SAIC Frederick, Frederick, MD 21702 USA.;Figg, WD, NCI, Mol Pharmacol Sect, Med Oncol Branch, Ctr Canc Res, 9000 Rockville Pike,Bldg 10,Room 5A01, Bethesda, MD 20892 USA.;Sissungt@mail.nih.gov baumcai@mail.nih.gov kirklandct@mail.nih.gov gaor@mail.nih.gov gardnerer@mail.nih.gov wdfigg@helix.nih.gov
    1. Year: 2010
    2. Date: Feb
  2. Journal: Molecular Biotechnology
    1. 44
    2. 2
    3. Pages: 152-167
  4. Type of Article: Review
  5. ISSN: 1073-6085
  1. Abstract:

    This review provides an overview of the pharmacogenetics of membrane transporters including selected ABC transporters (ABCB1, ABCC1, ABCC2, and ABCG2) and OATPs (OATP1B1 and OATP1B3). Membrane transporters are heavily involved in drug clearance and alters drug disposition by actively transporting substrate drugs between organs and tissues. As such, polymorphisms in the genes encoding these proteins may have significant effects on the absorption, distribution, metabolism and excretion of compounds, and may alter pharmacodynamics of many agents. This review discusses the techniques used to identify substrates and inhibitors of these proteins and subsequently to assess the effect of genetic mutation on transport, both in vitro and in vivo. A comprehensive list of substrates for the major drug transporters is included. Finally, studies linking transporter genotype with clinical outcomes are discussed.

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External Sources

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  2. DOI: 10.1007/s12033-009-9220-6
  3. View record in Web of Science®
  4. WOS: 000273675100010

Library Notes

  1. Fiscal Year: FY2009-2010
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