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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
The SLCO superfamily is comprised of the organic anion transporting polypeptides (OATPs). The 11 human OATPs are divided into 6 families and ten subfamilies based on amino acid identity. These proteins are located on the plasma membrane of cells throughout the body. They have 12 TM domains and intracellular termini, with multiple putative glycosylation sites. OATPs mediate the sodium-independent uptake of a wide range of amphiphilic substrates, including many drugs and toxins. Due to the multispecificity of these proteins, this guide lists classes of substrates and inhibitors for each family member. More comprehensive lists of substrates, inhibitors, and their relative affinities may be found in the review articles listed below.
* Key recommended reading is highlighted with an asterisk
* Gong IY, Kim RB. (2013) Impact of genetic variation in OATP transporters to drug disposition and response. Drug Metab. Pharmacokinet., 28 (1): 4-18. [PMID:23047721]
Hagenbuch B. (2010) Drug uptake systems in liver and kidney: a historic perspective. Clin. Pharmacol. Ther., 87 (1): 39-47. [PMID:19924123]
* Hagenbuch B, Stieger B. (2013) The SLCO (former SLC21) superfamily of transporters. Mol. Aspects Med., 34 (2-3): 396-412. [PMID:23506880]
König J. (2011) Uptake transporters of the human OATP family: molecular characteristics, substrates, their role in drug-drug interactions, and functional consequences of polymorphisms. Handb Exp Pharmacol, (201): 1-28. [PMID:21103967]
* König J, Müller F, Fromm MF. (2013) Transporters and drug-drug interactions: important determinants of drug disposition and effects. Pharmacol. Rev., 65 (3): 944-66. [PMID:23686349]
Niemi M, Pasanen MK, Neuvonen PJ. (2011) Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol. Rev., 63 (1): 157-81. [PMID:21245207]
* Obaidat A, Roth M, Hagenbuch B. (2012) The expression and function of organic anion transporting polypeptides in normal tissues and in cancer. Annu. Rev. Pharmacol. Toxicol., 52: 135-51. [PMID:21854228]
* Roth M, Obaidat A, Hagenbuch B. (2012) OATPs, OATs and OCTs: the organic anion and cation transporters of the SLCO and SLC22A gene superfamilies. Br. J. Pharmacol., 165 (5): 1260-87. [PMID:22013971]
* Shitara Y, Maeda K, Ikejiri K, Yoshida K, Horie T, Sugiyama Y. (2013) Clinical significance of organic anion transporting polypeptides (OATPs) in drug disposition: their roles in hepatic clearance and intestinal absorption. Biopharm Drug Dispos, 34 (1): 45-78. [PMID:23115084]
* Stieger B, Hagenbuch B. (2014) Organic anion-transporting polypeptides. Curr Top Membr, 73: 205-32. [PMID:24745984]
1. Bailey DG, Dresser GK, Leake BF, Kim RB. (2007) Naringin is a major and selective clinical inhibitor of organic anion-transporting polypeptide 1A2 (OATP1A2) in grapefruit juice. Clin. Pharmacol. Ther., 81 (4): 495-502. [PMID:17301733]
2. Chan BS, Satriano JA, Pucci M, Schuster VL. (1998) Mechanism of prostaglandin E2 transport across the plasma membrane of HeLa cells and Xenopus oocytes expressing the prostaglandin transporter "PGT". J. Biol. Chem., 273 (12): 6689-97. [PMID:9506966]
3. Kanai N, Lu R, Satriano JA, Bao Y, Wolkoff AW, Schuster VL. (1995) Identification and characterization of a prostaglandin transporter. Science, 268 (5212): 866-9. [PMID:7754369]
4. Noé J, Portmann R, Brun ME, Funk C. (2007) Substrate-dependent drug-drug interactions between gemfibrozil, fluvastatin and other organic anion-transporting peptide (OATP) substrates on OATP1B1, OATP2B1, and OATP1B3. Drug Metab. Dispos., 35 (8): 1308-14. [PMID:17470528]
5. Treiber A, Schneiter R, Häusler S, Stieger B. (2007) Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil. Drug Metab. Dispos., 35 (8): 1400-7. [PMID:17496208]
Database page citation:
Bruno Hagenbuch. SLCO family of organic anion transporting polypeptides. Accessed on 04/10/2015. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=238.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: Transporters. Br J Pharmacol. 170: 1706–1796.