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<datestamp>2017-12-21</datestamp>
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<title lang=en>Drug Transporter Expression and Activity in Human Hepatoma HuH-7 Cells.</title>
<creator>Jouan, Elodie</creator>
<creator>Le Vee, Marc</creator>
<creator>Denizot, Claire</creator>
<creator>Parmentier, Yannick</creator>
<creator>Fardel, Olivier</creator>
<contributor>Structure Fédérative de Recherche en Biologie et Santé de Rennes ( Biosit : Biologie - Santé - Innovation Technologique )</contributor>
<contributor>Institut de recherche, santé, environnement et travail [Rennes] (Irset) ; Université d'Angers (UA) - Université des Antilles et de la Guyane (UAG) - Université de Rennes 1 (UR1) - École des Hautes Études en Santé Publique [EHESP] (EHESP) - Institut National de la Santé et de la Recherche Médicale (INSERM) - Structure Fédérative de Recherche en Biologie et Santé de Rennes ( Biosit : Biologie - Santé - Innovation Technologique )</contributor>
<contributor>Technologie Servier ; Technologie Servier</contributor>
<contributor>CHU Pontchaillou [Rennes]</contributor>
<description>International audience</description>
<source>Pharmaceutics</source>
<identifier>hal-01477210</identifier>
<identifier>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01477210</identifier>
<source>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01477210</source>
<source>Pharmaceutics, 2016, 9 (1), pp.3. 〈10.3390/pharmaceutics9010003〉</source>
<identifier>DOI : 10.3390/pharmaceutics9010003</identifier>
<relation>info:eu-repo/semantics/altIdentifier/doi/10.3390/pharmaceutics9010003</relation>
<identifier>PUBMED : 28036031</identifier>
<relation>info:eu-repo/semantics/altIdentifier/pmid/28036031</relation>
<language>en</language>
<subject>[SDV.EE] Life Sciences [q-bio]/Ecology, environment</subject>
<type>info:eu-repo/semantics/article</type>
<type>Journal articles</type>
<description lang=en>Human hepatoma cells may represent a valuable alternative to the use of human hepatocytes for studying hepatic drug transporters, which is now a regulatory issue during drug development. In the present work, we have characterized hepatic drug transporter expression, activity and regulation in human hepatoma HuH-7 cells, in order to determine the potential relevance of these cells for drug transport assays. HuH-7 cells displayed notable multidrug resistance-associated protein (MRP) activity, presumed to reflect expression of various hepatic MRPs, including MRP2. By contrast, they failed to display functional activities of the uptake transporters sodium taurocholate co-transporting polypeptide (NTCP), organic anion-transporting polypeptides (OATPs) and organic cation transporter 1 (OCT1), and of the canalicular transporters P-glycoprotein and breast cancer resistance protein (BCRP). Concomitantly, mRNA expressions of various sinusoidal and canalicular hepatic drug transporters were not detected (NTCP, OATP1B1, organic anion transporter 2 (OAT2), OCT1 and bile salt export pump) or were found to be lower (OATP1B3, OATP2B1, multidrug and toxin extrusion protein 1, BCRP and MRP3) in hepatoma HuH-7 cells than those found in human hepatocytes, whereas other transporters such as OAT7, MRP4 and MRP5 were up-regulated. HuH-7 cells additionally exhibited farnesoid X receptor (FXR)- and nuclear factor erythroid</description>
<date>2016</date>
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