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Review
. 2015 May;17(3):535-45.
doi: 10.1208/s12248-015-9740-x. Epub 2015 Mar 4.

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

Nilay Thakkar  1 , A Craig Lockhart, Wooin Lee
Affiliations
Review

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

Nilay Thakkar et al. AAPS J. 2015 May.

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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References

    1. Hagenbuch B, Meier PJ. Organic anion transporting polypeptides of the OATP/ SLC21 family: phylogenetic classification as OATP/ SLCO superfamily, new nomenclature and molecular/functional properties. Pflugers Arch. 2004;447(5):653–65. doi: 10.1007/s00424-003-1168-y. - DOI - PubMed
    1. Abe T, Kakyo M, Tokui T, Nakagomi R, Nishio T, Nakai D, et al. Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1. J Biol Chem. 1999;274(24):17159–63. doi: 10.1074/jbc.274.24.17159. - DOI - PubMed
    1. Abe T, Unno M, Onogawa T, Tokui T, Kondo TN, Nakagomi R, et al. LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology. 2001;120(7):1689–99. doi: 10.1053/gast.2001.24804. - DOI - PubMed
    1. Lee W, Belkhiri A, Lockhart AC, Merchant N, Glaeser H, Harris EI, et al. Overexpression of OATP1B3 confers apoptotic resistance in colon cancer. Cancer Res. 2008;68(24):10315–23. doi: 10.1158/0008-5472.CAN-08-1984. - DOI - PMC - PubMed
    1. Olszewski-Hamilton U, Svoboda M, Thalhammer T, Buxhofer-Ausch V, Geissler K, Hamilton G. Organic anion transporting polypeptide 5A1 (OATP5A1) in small cell lung cancer (SCLC) cells: possible involvement in chemoresistance to satraplatin. Biomark Cancer. 2011;3:31–40. doi: 10.4137/BIC.S7151. - DOI - PMC - PubMed

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