ArticleAmerican journal of physiology. Gastrointestinal and liver physiology2008
Expression and hepatobiliary transport characteristics of the concentrative and equilibrative nucleoside transporters in sandwich-cultured human hepatocytes.
Article in American journal of physiology. Gastrointestinal and liver physiology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 73 citations in OpenAlex.
- Addressing the Clinical Importance of Equilibrative Nucleoside Transporters in Drug Discovery and Development.Clinical pharmacology and therapeutics · 2023Review
- Review of Transporter Substrate, Inhibitor, and Inducer Characteristics of Cladribine.Clinical pharmacokinetics · 2021Review
- Evaluation of Drug Biliary Excretion Using Sandwich-Cultured Human Hepatocytes.European journal of drug metabolism and pharmacokinetics · 2019Review
- mRNA Expression and Activity of Nucleoside Transporters in Human Hepatoma HepaRG Cells.Pharmaceutics · 2018Article
- A Cell Culture Platform to Maintain Long-term Phenotype of Primary Human Hepatocytes and Endothelial Cells.Cellular and molecular gastroenterology and hepatology · 2018Article
- Who Is Who in Adenosine Transport.Frontiers in pharmacology · 2018Review
- Article
- Equilibrative nucleoside transporter 1 expression in primary human hepatocytes is highly variable and determines uptake of ribavirin.Antiviral chemistry & chemotherapy · 2017Article
- The role of the equilibrative nucleoside transporter 1 on tissue and fetal distribution of ribavirin in the mouse.Biopharmaceutics & drug disposition · 2016Article
- Nucleoside transporter proteins as biomarkers of drug responsiveness and drug targets.Frontiers in pharmacology · 2015Review
- Nucleoside transporters and human organic cation transporter 1 determine the cellular handling of DNA-methyltransferase inhibitors.British journal of pharmacology · 2014Article
- Effects of chronic kidney disease and uremia on hepatic drug metabolism and transport.Kidney international · 2014Review
- Bile formation and secretion.Comprehensive Physiology · 2013Review
- Interaction between HIV protease inhibitors (PIs) and hepatic transporters in sandwich cultured human hepatocytes: implication for PI-based DDIs.Biopharmaceutics & drug disposition · 2013Article
- Article
- Article
- Role of the equilibrative and concentrative nucleoside transporters in the intestinal absorption of the nucleoside drug, ribavirin, in wild-type and Ent1(-/-) mice.Molecular pharmaceutics · 2012Article
- CNT1 expression influences proliferation and chemosensitivity in drug-resistant pancreatic cancer cells.Cancer research · 2011Article
- Sandwich-cultured hepatocytes: an in vitro model to evaluate hepatobiliary transporter-based drug interactions and hepatotoxicity.Drug metabolism reviews · 2010Review
- Influence of seeding density and extracellular matrix on bile Acid transport and mrp4 expression in sandwich-cultured mouse hepatocytes.Molecular pharmaceutics · 2010Article
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Authors and funding
7 authors at 4 institutions in 3 countries.
Funding
Abstract
We previously reported that both the concentrative (hCNT) and equilibrative (hENT) nucleoside transporters are expressed in the human liver (21). Here we report a study that investigated the expression of these transporters (transcripts and proteins) and their role in the hepatobiliary transport of nucleosides/nucleoside drugs using sandwich-cultured human hepatocytes. In the hepatic tissue, the rank order of the mRNA expression of the transporters was hCNT1 approximately hENT1>hENT2 approximately hCNT2>hCNT3. In sandwich-cultured hepatocytes, the mRNA expression of hCNT2 and hENT2 was comparable to that in hepatic tissue, whereas the expression of corresponding transporters in the two-dimensional hepatocyte cultures was lower. Colocalization studies demonstrated predominant localization of these transporters at the sinusoidal membrane and of hENT1, hCNT1, and hCNT2 at the canalicular membrane. In the sandwich-cultured hepatocytes, ENTs were the major contributors to the transport of thymidine (hENT1, 63%; hENT2, 23%) or guanosine (hENT1, 53%; hENT2, 24%) into the hepatocytes followed by hCNT1 (10%) for thymidine or hCNT2 (23%) for guanosine. Although ribavirin was predominately transported (89%) into the hepatocytes by hENT1, fialuridine (FIAU) was transported by both hENT1 (30%) and hCNTs (61%). The extensively metabolized natural nucleosides were not effluxed into the bile, whereas significant biliary-efflux was observed of FIAU (19%), ribavirin (30%), and formycin B (35%). We conclude that the hepatic activity of hENT1 and hCNT1/2 transporters will determine the in vivo hepatic distribution and therefore the efficacy and/or toxicity of nucleoside drugs used to treat hepatic diseases.
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