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Drug Transporter Expression and Activity in Human Hepatoma HuH-7 Cells.

Abstract : 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
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https://hal-univ-rennes1.archives-ouvertes.fr/hal-01477210
Contributor : Xavier Chard-Hutchinson <>
Submitted on : Monday, February 27, 2017 - 10:39:02 AM
Last modification on : Thursday, April 30, 2020 - 10:48:25 AM

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Elodie Jouan, Marc Le Vee, Claire Denizot, Yannick Parmentier, Olivier Fardel. Drug Transporter Expression and Activity in Human Hepatoma HuH-7 Cells.. Pharmaceutics, 2017, 9 (1), pp.3. ⟨10.3390/pharmaceutics9010003⟩. ⟨hal-01477210⟩

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