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Role of Organic Anion-Transporting Polypeptides (OATPs) in Cancer Therapy

  • Review Article
  • Theme: Transporters and Cancer Therapy
  • Published:
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Abstract

The superfamily of organic anion-transporting polypeptides (OATPs, gene symbol SLCO) includes important transporters handling a variety of endogenous and xenobiotic substrates. Currently, 11 human OATPs are known and their substrates include endogenous hormones and their conjugates, anticancer drugs, and imaging agents. The contribution of OATPs to the in vivo disposition of these substrates has been extensively investigated. An accumulating body of evidence also indicates that the expression of some OATPs may be up- or downregulated in several types of cancers, suggesting potential pathogenic roles during the development and progression of cancer. Given that the role of OATPs in handling cancer therapeutics has been already covered by several excellent reviews, this review will focus on the recent progresses on the topic, in particular the role of OATPs in the disposition of anticancer drugs, the impact of OATP genetic variations on the function of OATPs, and the OATPs differentially expressed in cancer and their potential roles in cancer development, progression, and treatment.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky, USA

    Nilay Thakkar & Wooin Lee

  2. Department of Medicine, Washington University School of Medicine, St. Louis, Missouri, USA

    A. Craig Lockhart

  3. College of Pharmacy, Seoul National University, Seoul, South Korea

    Wooin Lee

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  1. Nilay Thakkar
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  2. A. Craig Lockhart
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  3. Wooin Lee
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Correspondence to Wooin Lee.

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Guest Editor: Rajgopal Govindarajan

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Thakkar, N., Lockhart, A.C. & Lee, W. Role of Organic Anion-Transporting Polypeptides (OATPs) in Cancer Therapy. AAPS J 17, 535–545 (2015). https://doi.org/10.1208/s12248-015-9740-x

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