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Gene Review

SLCO4A1  -  solute carrier organic anion transporter...

Homo sapiens

Synonyms: Colon organic anion transporter, OATP-E, OATP-RP1, OATP1, OATP4A1, ...
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Disease relevance of SLCO4A1

  • Inhibition of human organic anion transporting polypeptide OATP 1B1 as a mechanism of drug-induced hyperbilirubinemia [1].
  • We characterized the interaction of MTX with human organic-anion transporting polypeptide transporter (OATP) 1A2, which is expressed in tissues important for MTX disposition and toxicity, such as the intestine, kidney, liver, and endothelial cells of the blood-brain barrier [2].
  • OATP expression, determined by immunoblotting, was similar in hepatocellular carcinomas and surrounding liver tissue (n = 3) [3].
  • Uptake of the cytostatic drug [3H]-chlorambucil-taurocholate (S2676) was measured in Xenopus laevis oocytes injected with total messenger RNA (mRNA) from the carcinomas or peritumor tissue or with complementary RNA encoding the NTCP or the organic anion-transporting polypeptide (OATP) of human liver [3].
  • Reverse-transcription polymerase chain reaction analysis showed an increase in OATP messenger RNA in the livers of four patients with chronic cholestatic liver disease compared with three noncholestatic controls [4].

High impact information on SLCO4A1

  • Among them, cephalosporins and probenecid have the potential to produce clinically relevant OAT-mediated drug-drug interactions, whereas cyclosporin A and rifampicin may trigger OATP-mediated ones [5].
  • Human organic anion transporting polypeptide (OATP) 1B1 and sodium-dependent taurocholate cotransporting polypeptide (NTCP) allelic variants were also assessed [6].
  • RESULTS: Multiple OATP family members, including 1B1, 1B3, 2B1, and 1A2, were capable of rosuvastatin transport [6].
  • Transport of 16 substrates was measured for each individual human OATP in complementary RNA-injected Xenopus laevis oocytes [7].
  • Although most of the tested compounds are common substrates of several oatp-related transporters, high-affinity uptake of digoxin is a unique feature of the newly cloned oatp2 [8].

Chemical compound and disease context of SLCO4A1


Biological context of SLCO4A1


Anatomical context of SLCO4A1


Associations of SLCO4A1 with chemical compounds


Other interactions of SLCO4A1

  • In rats, rifamycin SV and rifampicin were shown to interfere with hepatic organic anion uptake by inhibition of the organic anion transporting polypeptides Oatp1 and Oatp2 [20].
  • The specific activity of OATP-B per mRNA expression was much higher than that of OATP-D and OATP-E [13].
  • This study localizes the human OATP (now called OATP-A; SLC21A3) at the BBB in humans [15].
  • In vitro, atorvastatin acid is a substrate for P-glycoprotein, organic anion-transporting polypeptide (OATP) C and H+-monocarboxylic acid cotransporter [21].

Analytical, diagnostic and therapeutic context of SLCO4A1


  1. Inhibition of human organic anion transporting polypeptide OATP 1B1 as a mechanism of drug-induced hyperbilirubinemia. Campbell, S.D., de Morais, S.M., Xu, J.J. Chem. Biol. Interact. (2004) [Pubmed]
  2. Interaction of methotrexate with organic-anion transporting polypeptide 1A2 and its genetic variants. Badagnani, I., Castro, R.A., Taylor, T.R., Brett, C.M., Huang, C.C., Stryke, D., Kawamoto, M., Johns, S.J., Ferrin, T.E., Carlson, E.J., Burchard, E.G., Giacomini, K.M. J. Pharmacol. Exp. Ther. (2006) [Pubmed]
  3. Chlorambucil-taurocholate is transported by bile acid carriers expressed in human hepatocellular carcinomas. Kullak-Ublick, G.A., Glasa, J., Böker, C., Oswald, M., Grützner, U., Hagenbuch, B., Stieger, B., Meier, P.J., Beuers, U., Kramer, W., Wess, G., Paumgartner, G. Gastroenterology (1997) [Pubmed]
  4. Identification and functional characterization of the promoter region of the human organic anion transporting polypeptide gene. Kullak-Ublick, G.A., Beuers, U., Fahney, C., Hagenbuch, B., Meier, P.J., Paumgartner, G. Hepatology (1997) [Pubmed]
  5. Evaluation of drug-drug interaction in the hepatobiliary and renal transport of drugs. Shitara, Y., Sato, H., Sugiyama, Y. Annu. Rev. Pharmacol. Toxicol. (2005) [Pubmed]
  6. Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Ho, R.H., Tirona, R.G., Leake, B.F., Glaeser, H., Lee, W., Lemke, C.J., Wang, Y., Kim, R.B. Gastroenterology (2006) [Pubmed]
  7. Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Kullak-Ublick, G.A., Ismair, M.G., Stieger, B., Landmann, L., Huber, R., Pizzagalli, F., Fattinger, K., Meier, P.J., Hagenbuch, B. Gastroenterology (2001) [Pubmed]
  8. Isolation of a multispecific organic anion and cardiac glycoside transporter from rat brain. Noé, B., Hagenbuch, B., Stieger, B., Meier, P.J. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  9. Active influx transport is mediated by members of the organic anion transporting polypeptide family in human epidermal keratinocytes. Schiffer, R., Neis, M., Höller, D., Rodríguez, F., Geier, A., Gartung, C., Lammert, F., Dreuw, A., Zwadlo-Klarwasser, G., Merk, H., Jugert, F., Baron, J.M. J. Invest. Dermatol. (2003) [Pubmed]
  10. A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane. König, J., Cui, Y., Nies, A.T., Keppler, D. Am. J. Physiol. Gastrointest. Liver Physiol. (2000) [Pubmed]
  11. Orange juice increased the bioavailability of pravastatin, 3-hydroxy-3-methylglutaryl CoA reductase inhibitor, in rats and healthy human subjects. Koitabashi, Y., Kumai, T., Matsumoto, N., Watanabe, M., Sekine, S., Yanagida, Y., Kobayashi, S. Life Sci. (2006) [Pubmed]
  12. Localization of organic anion transporting polypeptides in the rat and human ciliary body epithelium. Gao, B., Huber, R.D., Wenzel, A., Vavricka, S.R., Ismair, M.G., Remé, C., Meier, P.J. Exp. Eye Res. (2005) [Pubmed]
  13. Predominant contribution of organic anion transporting polypeptide OATP-B (OATP2B1) to apical uptake of estrone-3-sulfate by human intestinal Caco-2 cells. Sai, Y., Kaneko, Y., Ito, S., Mitsuoka, K., Kato, Y., Tamai, I., Artursson, P., Tsuji, A. Drug Metab. Dispos. (2006) [Pubmed]
  14. The organic anion transport polypeptide 1d1 (Oatp1d1) mediates hepatocellular uptake of phalloidin and microcystin into skate liver. Meier-Abt, F., Hammann-Hänni, A., Stieger, B., Ballatori, N., Boyer, J.L. Toxicol. Appl. Pharmacol. (2007) [Pubmed]
  15. Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier. Gao, B., Hagenbuch, B., Kullak-Ublick, G.A., Benke, D., Aguzzi, A., Meier, P.J. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  16. A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. Hsiang, B., Zhu, Y., Wang, Z., Wu, Y., Sasseville, V., Yang, W.P., Kirchgessner, T.G. J. Biol. Chem. (1999) [Pubmed]
  17. Identification of thyroid hormone transporters in humans: different molecules are involved in a tissue-specific manner. Fujiwara, K., Adachi, H., Nishio, T., Unno, M., Tokui, T., Okabe, M., Onogawa, T., Suzuki, T., Asano, N., Tanemoto, M., Seki, M., Shiiba, K., Suzuki, M., Kondo, Y., Nunoki, K., Shimosegawa, T., Iinuma, K., Ito, S., Matsuno, S., Abe, T. Endocrinology (2001) [Pubmed]
  18. Organic anion transporting polypeptides expressed in liver and brain mediate uptake of microcystin. Fischer, W.J., Altheimer, S., Cattori, V., Meier, P.J., Dietrich, D.R., Hagenbuch, B. Toxicol. Appl. Pharmacol. (2005) [Pubmed]
  19. Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. Shimizu, M., Fuse, K., Okudaira, K., Nishigaki, R., Maeda, K., Kusuhara, H., Sugiyama, Y. Drug Metab. Dispos. (2005) [Pubmed]
  20. Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Vavricka, S.R., Van Montfoort, J., Ha, H.R., Meier, P.J., Fattinger, K. Hepatology (2002) [Pubmed]
  21. Clinical pharmacokinetics of atorvastatin. Lennernäs, H. Clinical pharmacokinetics. (2003) [Pubmed]
  22. Identification of steroid sulfate transport processes in the human mammary gland. Pizzagalli, F., Varga, Z., Huber, R.D., Folkers, G., Meier, P.J., St-Pierre, M.V. J. Clin. Endocrinol. Metab. (2003) [Pubmed]
  23. Molecular and functional characterization of bile acid transport in human hepatoblastoma HepG2 cells. Kullak-Ublick, G.A., Beuers, U., Paumgartner, G. Hepatology (1996) [Pubmed]
  24. Assignment of the human organic anion transporting polypeptide (OATP) gene to chromosome 12p12 by fluorescence in situ hybridization. Kullak-Ublick, G.A., Beuers, U., Meier, P.J., Domdey, H., Paumgartner, G. J. Hepatol. (1996) [Pubmed]
  25. Expression of organic anion transporting polypeptide E (OATP-E) in human placenta. Sato, K., Sugawara, J., Sato, T., Mizutamari, H., Suzuki, T., Ito, A., Mikkaichi, T., Onogawa, T., Tanemoto, M., Unno, M., Abe, T., Okamura, K. Placenta (2003) [Pubmed]
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