PMID: 8938553Nov 1, 1996Paper

Multispecific amphipathic substrate transport by an organic anion transporter of human liver

Journal of Hepatology
X BossuytP J Meier

Abstract

Hepatic uptake of differently charged amphipathic endo- and xenobiotics is thought to occur via distinct carrier-mediated transport systems. Alternatively, a single rat organic anion transporting polypeptide (oatp) has recently been demonstrated to mediate hepatocellular uptake of differently charged amphipathic substrates. To investigate whether a cloned human liver organic anion transporting polypeptide (OATP) also can mediate charge- and class-independent hepatocellular uptake of amphipathic substrates. Xenopus laevis oocytes were injected with OATP-cRNA. Sodium-independent uptake of estrone-3-sulfate, ouabain and the organic cation N-(4,4-azo-n-pentyl)-21-ajmalinium was compared in OATP-expressing and uninjected (or water injected) control oocytes. Our results indicate that OATP, in addition to bromosulfophthalein and bile salts, can also transport anionic estrone-3-sulfate (Km approximately 59 microM), neutral ouabain (K(m) approximately 5.5 mM) and cationic N-(4,4-azo-n-pentyl)-21-ajmalinium. For each of these compounds, OATP-mediated uptake was cis-inhibited by the OATP substrate taurochenodeoxycholate and the transport activities correlated well with the amounts of cRNA injected. Similar to the rat liver oatp, the human...Continue Reading

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Citations

Oct 31, 1998·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·K S PangA W Wolkoff
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Mar 10, 2006·Naunyn-Schmiedeberg's Archives of Pharmacology·Jörg KönigMartin F Fromm
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