equilibrative nucleoside transporter 1

Summary

Summary: A subtype of equilibrative nucleoside transporter proteins that is sensitive to inhibition by 4-nitrobenzylthioinosine.

Top Publications

  1. Marechal R, Bachet J, Mackey J, Dalban C, Demetter P, Graham K, et al. Levels of gemcitabine transport and metabolism proteins predict survival times of patients treated with gemcitabine for pancreatic adenocarcinoma. Gastroenterology. 2012;143:664-674.e6 pubmed publisher
    ..Key determinants of gemcitabine cytotoxicity include the activities of the human equilibrative nucleoside transporter 1 (hENT1), deoxycytidine kinase (dCK), and ribonucleotide reductase subunit 1 (RRM1)...
  2. Yao S, Ng A, Cass C, Baldwin S, Young J. Nucleobase transport by human equilibrative nucleoside transporter 1 (hENT1). J Biol Chem. 2011;286:32552-62 pubmed publisher
    ..Site-directed mutagenesis identified Cys-414 in transmembrane helix 10 of hENT1 as the residue conferring nucleobase transport activity to the wild-type transporter. ..
  3. Sengupta D, Lum P, Lai Y, Shubochkina E, Bakken A, Schneider G, et al. A single glycine mutation in the equilibrative nucleoside transporter gene, hENT1, alters nucleoside transport activity and sensitivity to nitrobenzylthioinosine. Biochemistry. 2002;41:1512-9 pubmed
    ..This is the first identification and characterization of a critical amino acid residue of hENT1 that is important in both nucleoside transporter function and sensitivity to inhibition by NBMPR. ..
  4. Pennycooke M, Chaudary N, Shuralyova I, Zhang Y, Coe I. Differential expression of human nucleoside transporters in normal and tumor tissue. Biochem Biophys Res Commun. 2001;280:951-9 pubmed
    ..Decreased NT expression in tumor tissue may contribute to reduced drug uptake and the development of resistance. These data suggest that nucleoside analog drug therapies may be optimized by determining individual NT expression profiles. ..
  5. Visser F, Sun L, Damaraju V, Tackaberry T, Peng Y, Robins M, et al. Residues 334 and 338 in transmembrane segment 8 of human equilibrative nucleoside transporter 1 are important determinants of inhibitor sensitivity, protein folding, and catalytic turnover. J Biol Chem. 2007;282:14148-57 pubmed
    ..Human equilibrative nucleoside transporter 1 (hENT1) is inhibited by nanomolar concentrations of structurally diverse compounds, including ..
  6. Nam H, Lee M, Hinton D, Choi D. Reduced effect of NMDA glutamate receptor antagonist on ethanol-induced ataxia and striatal glutamate levels in mice lacking ENT1. Neurosci Lett. 2010;479:277-81 pubmed publisher
    ..Our findings suggest that differential glutamate neurotransmission in the striatum regulates ethanol intoxication. ..
  7. Spratlin J, Sangha R, Glubrecht D, Dabbagh L, Young J, Dumontet C, et al. The absence of human equilibrative nucleoside transporter 1 is associated with reduced survival in patients with gemcitabine-treated pancreas adenocarcinoma. Clin Cancer Res. 2004;10:6956-61 pubmed
    ..In vitro studies have demonstrated that deficiency of human equilibrative nucleoside transporter 1 (hENT1), the most widely abundant and distributed nucleoside transporter in human cells, confers ..
  8. Coe I, Zhang Y, McKenzie T, Naydenova Z. PKC regulation of the human equilibrative nucleoside transporter, hENT1. FEBS Lett. 2002;517:201-5 pubmed
    ..protein kinase C (PKC) causes a rapid increase in S-(4-nitrobenzyl)-6-thioinosine-sensitive (human equilibrative nucleoside transporter 1, hENT1) nucleoside uptake, in human cultured cells, which is not due to increased metabolism and ..
  9. Stam R, den Boer M, Meijerink J, Ebus M, Peters G, Noordhuis P, et al. Differential mRNA expression of Ara-C-metabolizing enzymes explains Ara-C sensitivity in MLL gene-rearranged infant acute lymphoblastic leukemia. Blood. 2003;101:1270-6 pubmed
    ..026) but 2.5-fold more mRNA of the equilibrative nucleoside transporter 1 (hENT1), responsible for Ara-C membrane transport (P =.001)...

More Information

Publications73

  1. Ohhashi S, Ohuchida K, Mizumoto K, Fujita H, Egami T, Yu J, et al. Down-regulation of deoxycytidine kinase enhances acquired resistance to gemcitabine in pancreatic cancer. Anticancer Res. 2008;28:2205-12 pubmed
    ..The hENT-targeting siRNA did not affect gemcitabine sensitivity or cell proliferation. Down-regulation of dCK specifically enhanced acquired resistance to gemcitabine in pancreatic cancer cells without affecting their proliferation. ..
  2. Kim S, Saito Y, Maekawa K, Sugiyama E, Kaniwa N, Ueno H, et al. Thirty novel genetic variations in the SLC29A1 gene encoding human equilibrative nucleoside transporter 1 (hENT1). Drug Metab Pharmacokinet. 2006;21:248-56 pubmed
    ..variations, including thirty novel ones, were found in the human SLC29A1 gene, which encodes equilibrative nucleoside transporter 1, from 256 Japanese cancer patients administered gemcitabine...
  3. Wu J, Lee M, Choi S, Kim T, Choi D. ENT1 regulates ethanol-sensitive EAAT2 expression and function in astrocytes. Alcohol Clin Exp Res. 2010;34:1110-7 pubmed publisher
    b>Equilibrative nucleoside transporter 1 (ENT1) and excitatory amino acid transporter 2 (EAAT2) are predominantly expressed in astrocytes where they are thought to regulate synaptic adenosine and glutamate levels...
  4. Choi D, Cascini M, Mailliard W, Young H, Paredes P, McMahon T, et al. The type 1 equilibrative nucleoside transporter regulates ethanol intoxication and preference. Nat Neurosci. 2004;7:855-61 pubmed
    ..Our results indicate that ENT1 has a physiological role in ethanol-mediated behaviors and suggest that decreased A(1) adenosine receptor function promotes alcohol consumption. ..
  5. Pérez Torras S, García Manteiga J, Mercade E, Casado F, Carbó N, Pastor Anglada M, et al. Adenoviral-mediated overexpression of human equilibrative nucleoside transporter 1 (hENT1) enhances gemcitabine response in human pancreatic cancer. Biochem Pharmacol. 2008;76:322-9 pubmed publisher
    ..In summary, hENT1 overexpression is associated with alterations in nucleoside enzymatic machinery and cell cycle progression in cultured cells and enhances gemcitabine action in vivo. ..
  6. Abdulla P, Coe I. Characterization and functional analysis of the promoter for the human equilibrative nucleoside transporter gene, hENT1. Nucleosides Nucleotides Nucleic Acids. 2007;26:99-110 pubmed
    ..Putative consensus sites for transcription factors exist within the hENT1 promoter. Reporter assays revealed similar but not identical transcriptional activity profiles in human cells. ..
  7. Escudero C, Casanello P, Sobrevia L. Human equilibrative nucleoside transporters 1 and 2 may be differentially modulated by A2B adenosine receptors in placenta microvascular endothelial cells from pre-eclampsia. Placenta. 2008;29:816-25 pubmed publisher
    ..Thus, A2B adenosine receptors may differentially modulate hENTs in hPMEC, which could be a mechanism attempting to re-establish physiological extracellular adenosine levels in pre-eclampsia. ..
  8. Perrone G, Morini S, Santini D, Rabitti C, Vincenzi B, Alloni R, et al. Human equilibrative nucleoside transporter 1 and carcinoma of the ampulla of Vater: expression differences in tumour histotypes. Eur J Histochem. 2010;54:e38 pubmed
    The human equilibrative nucleoside transporter 1 (hENT1) is the major means by which gemcitabine enters human cells; recent evidence exists that hENT1 is expressed in carcinoma of the ampulla of Vater and that it should be considered as a ..
  9. Guillen Gomez E, Pinilla Macua I, Pérez Torras S, Choi D, Arce Y, Ballarín J, et al. New role of the human equilibrative nucleoside transporter 1 (hENT1) in epithelial-to-mesenchymal transition in renal tubular cells. J Cell Physiol. 2012;227:1521-8 pubmed publisher
    ..b>Equilibrative nucleoside transporter 1 (ENT1) has been proved to be the most widely expressed adenosine transporter...
  10. Leisewitz A, Zimmerman E, Huang M, Jones S, Yang J, Graves L. Regulation of ENT1 expression and ENT1-dependent nucleoside transport by c-Jun N-terminal kinase. Biochem Biophys Res Commun. 2011;404:370-5 pubmed publisher
    ..We propose that activation of JNK-cJun pathway negatively regulates mENT1 and suggest that this mechanism might contribute to the development of nucleoside analog-derived drug resistance. ..
  11. Endres C, Moss A, Ke B, Govindarajan R, Choi D, Messing R, et al. The role of the equilibrative nucleoside transporter 1 (ENT1) in transport and metabolism of ribavirin by human and wild-type or Ent1-/- mouse erythrocytes. J Pharmacol Exp Ther. 2009;329:387-98 pubmed publisher
    ..We predict that Ent1(+/+) and Ent1(-/-) mice will serve as excellent models to investigate the contribution of Ent1 to the pharmacokinetics and toxicity of ribavirin in vivo. ..
  12. Rose J, Naydenova Z, Bang A, Ramadan A, Klawitter J, Schram K, et al. Absence of equilibrative nucleoside transporter 1 in ENT1 knockout mice leads to altered nucleoside levels following hypoxic challenge. Life Sci. 2011;89:621-30 pubmed publisher
    ..ENT1-null mice possess elevated circulating adenosine levels and reduced cellular uptake resulting in a perpetually cardioprotected phenotype. ..
  13. Kondo N, Murakami Y, Uemura K, Sudo T, Hashimoto Y, Nakashima A, et al. Combined analysis of dihydropyrimidine dehydrogenase and human equilibrative nucleoside transporter 1 expression predicts survival of pancreatic carcinoma patients treated with adjuvant gemcitabine plus S-1 chemotherapy after surgical resection. Ann Surg Oncol. 2012;19 Suppl 3:S646-55 pubmed publisher
    ..this study was to investigate whether intratumoral dihydropyrimidine dehydrogenase (DPD) and human equilibrative nucleoside transporter 1 (hENT1) expression can predict the survival of PDAC patients treated with adjuvant gemcitabine ..
  14. Sengupta D, Unadkat J. Glycine 154 of the equilibrative nucleoside transporter, hENT1, is important for nucleoside transport and for conferring sensitivity to the inhibitors nitrobenzylthioinosine, dipyridamole, and dilazep. Biochem Pharmacol. 2004;67:453-8 pubmed
    ..Collectively, these results suggest that glycine 154 plays an important role in the transport of nucleosides and in sensitivity to the inhibitors NBMPR, DP, and DZ. ..
  15. Farias M, Puebla C, Westermeier F, Jo M, Pastor Anglada M, Casanello P, et al. Nitric oxide reduces SLC29A1 promoter activity and adenosine transport involving transcription factor complex hCHOP-C/EBPalpha in human umbilical vein endothelial cells from gestational diabetes. Cardiovasc Res. 2010;86:45-54 pubmed publisher
    Reduced expression of human equilibrative nucleoside transporter 1 (hENT1) results from nitric oxide (NO)-dependent reduced SLC29A1 transcriptional activity in human umbilical vein endothelial cells (HUVECs) from gestational diabetes...
  16. Warraich S, Bone D, Quinonez D, Ii H, Choi D, Holdsworth D, et al. Loss of equilibrative nucleoside transporter 1 in mice leads to progressive ectopic mineralization of spinal tissues resembling diffuse idiopathic skeletal hyperostosis in humans. J Bone Miner Res. 2013;28:1135-49 pubmed publisher
    ..b>Equilibrative nucleoside transporter 1 (ENT1) transfers hydrophilic nucleosides, such as adenosine, across the plasma membrane...
  17. Farrell J, Elsaleh H, Garcia M, Lai R, Ammar A, Regine W, et al. Human equilibrative nucleoside transporter 1 levels predict response to gemcitabine in patients with pancreatic cancer. Gastroenterology. 2009;136:187-95 pubmed publisher
    ..These findings are supported by preclinical data; the gemcitabine transporter hENT1 is therefore a molecular and mechanistically relevant predictive marker of benefit from gemcitabine in patients with resected pancreatic cancer. ..
  18. Bernard C, Traub M, Kunz H, Hach S, Trentmann O, Möhlmann T. Equilibrative nucleoside transporter 1 (ENT1) is critical for pollen germination and vegetative growth in Arabidopsis. J Exp Bot. 2011;62:4627-37 pubmed publisher
    ..This indicates that ENT1-mediated nucleosides, especially adenosine transport, is important for nucleotide metabolism, thus influencing growth and pollen germination. ..
  19. Santini D, Schiavon G, Vincenzi B, Cass C, Vasile E, Manazza A, et al. Human equilibrative nucleoside transporter 1 (hENT1) levels predict response to gemcitabine in patients with biliary tract cancer (BTC). Curr Cancer Drug Targets. 2011;11:123-9 pubmed
    Translational data suggest that nucleoside transporters, in particular human equilibrative nucleoside transporter 1 (hENT1), play an important role in predicting clinical outcome after gemcitabine chemotherapy for several types of cancer...
  20. Marechal R, Mackey J, Lai R, Demetter P, Peeters M, Polus M, et al. Human equilibrative nucleoside transporter 1 and human concentrative nucleoside transporter 3 predict survival after adjuvant gemcitabine therapy in resected pancreatic adenocarcinoma. Clin Cancer Res. 2009;15:2913-9 pubmed publisher
    ..Human equilibrative nucleoside transporter 1 (hENT1) and human concentrative nucleoside transporter (hCNT) 1 and 3 are the major transporters ..
  21. Waidmann O, Pleli T, Dvorak K, Baehr C, Mondorf U, Plotz G, et al. Inhibition of the equilibrative nucleoside transporter 1 and activation of A2A adenosine receptors by 8-(4-chlorophenylthio)-modified cAMP analogs and their hydrolytic products. J Biol Chem. 2009;284:32256-63 pubmed publisher
    ..and 8-(4-chlorophenylthio)-2'-O-methyl-adenosine (8-pCPT-2'-O-methyl-ado)) inhibit the equilibrative nucleoside transporter 1 (ENT1)...
  22. Chen J, Nam H, Lee M, Hinton D, Choi S, Kim T, et al. Altered glutamatergic neurotransmission in the striatum regulates ethanol sensitivity and intake in mice lacking ENT1. Behav Brain Res. 2010;208:636-42 pubmed publisher
    ..Our results suggest that adenosine-regulated glutamatergic signaling contributes to a reduced level of alcohol response, which might be associated with a higher susceptibility for alcoholism in humans. ..
  23. Matsumura N, Nakamura Y, Kohjimoto Y, Inagaki T, Nanpo Y, Yasuoka H, et al. The prognostic significance of human equilibrative nucleoside transporter 1 expression in patients with metastatic bladder cancer treated with gemcitabine-cisplatin-based combination chemotherapy. BJU Int. 2011;108:E110-6 pubmed publisher
    To evaluate the expression of the human equilibrative nucleoside transporter 1 (hENT1) and excision repair cross complementing 1 (ERCC1) as possible prognostic factors for patients with metastatic bladder cancer treated with gemcitabine-..
  24. Zhang D, Xiong W, Albensi B, Parkinson F. Expression of human equilibrative nucleoside transporter 1 in mouse neurons regulates adenosine levels in physiological and hypoxic-ischemic conditions. J Neurochem. 2011;118:4-11 pubmed publisher
  25. Mori R, Ishikawa T, Ichikawa Y, Taniguchi K, Matsuyama R, Ueda M, et al. Human equilibrative nucleoside transporter 1 is associated with the chemosensitivity of gemcitabine in human pancreatic adenocarcinoma and biliary tract carcinoma cells. Oncol Rep. 2007;17:1201-5 pubmed
    ..Quantitative RT-PCR demonstrated that one of the nucleotide transporter genes; human equilibrative nucleoside transporter 1 (hENT1) was associated with the sensitivity to gemcitabine as represented by IC50, while the other ..
  26. Munoz G, San Martín R, Farias M, Cea L, Vecchiola A, Casanello P, et al. Insulin restores glucose inhibition of adenosine transport by increasing the expression and activity of the equilibrative nucleoside transporter 2 in human umbilical vein endothelium. J Cell Physiol. 2006;209:826-35 pubmed
  27. Casanello P, Torres A, Sanhueza F, Gonzalez M, Farias M, Gallardo V, et al. Equilibrative nucleoside transporter 1 expression is downregulated by hypoxia in human umbilical vein endothelium. Circ Res. 2005;97:16-24 pubmed
    ..These results could be important in diseases where the fetus is exposed to intrauterine environments poor in oxygen, such as intrauterine growth restriction, or where adenosine transport is altered, such as gestational diabetes. ..
  28. Takagaki K, Katsuma S, Kaminishi Y, Horio T, Nakagawa S, Tanaka T, et al. Gene-expression profiling reveals down-regulation of equilibrative nucleoside transporter 1 (ENT1) in Ara-C-resistant CCRF-CEM-derived cells. J Biochem. 2004;136:733-40 pubmed
    ..The adenosine deaminase (ADA) gene was highly up-regulated in Ara-C-resistant cells, while equilibrative nucleoside transporter 1 (ENT1) and several cell-cycle-related genes were down-regulated...
  29. Hammond J, Stolk M, Archer R, McConnell K. Pharmacological analysis and molecular cloning of the canine equilibrative nucleoside transporter 1. Eur J Pharmacol. 2004;491:9-19 pubmed
    ..These data indicate that the dog es/ENT1 transporter has distinctive inhibitor binding characteristics, and that these characteristics are a function of the protein structure as opposed to the environment in which it is expressed. ..
  30. Damaraju V, Mowles D, Yao S, Ng A, Young J, Cass C, et al. Role of human nucleoside transporters in the uptake and cytotoxicity of azacitidine and decitabine. Nucleosides Nucleotides Nucleic Acids. 2012;31:236-55 pubmed publisher
  31. Galmarini C, Thomas X, Calvo F, Rousselot P, El Jafaari A, Cros E, et al. Potential mechanisms of resistance to cytarabine in AML patients. Leuk Res. 2002;26:621-9 pubmed
    To determine whether the human equilibrative nucleoside transporter 1 (hENT1), deoxycytidine kinase (dCK), cytoplasmic 5'-nucleotidase (5NT), cytidine deaminase (CDD), topoisomerase I (TOPO I) and topoisomerase II alpha (TOPO II) are ..
  32. Mackey J, Jennings L, Clarke M, Santos C, Dabbagh L, Vsianska M, et al. Immunohistochemical variation of human equilibrative nucleoside transporter 1 protein in primary breast cancers. Clin Cancer Res. 2002;8:110-6 pubmed
  33. Griffiths M, Beaumont N, Yao S, Sundaram M, Boumah C, Davies A, et al. Cloning of a human nucleoside transporter implicated in the cellular uptake of adenosine and chemotherapeutic drugs. Nat Med. 1997;3:89-93 pubmed
  34. Fujita H, Ohuchida K, Mizumoto K, Itaba S, Ito T, Nakata K, et al. Gene expression levels as predictive markers of outcome in pancreatic cancer after gemcitabine-based adjuvant chemotherapy. Neoplasia. 2010;12:807-17 pubmed
  35. Xiao J, Zhang T, Zhao Y. Human equilibrative nucleoside transporter 1 (hENT1) predicts the Asian patient response to gemcitabine-based chemotherapy in pancreatic cancer. Hepatogastroenterology. 2013;60:258-62 pubmed publisher
    ..We studied the relationship between human equilibrative nucleoside transporter 1 (hENT1) expression in tumor cells and the Asian patient response to gemcitabine-based chemotherapy...
  36. Sugiyama E, Kaniwa N, Kim S, Hasegawa R, Saito Y, Ueno H, et al. Population pharmacokinetics of gemcitabine and its metabolite in Japanese cancer patients: impact of genetic polymorphisms. Clin Pharmacokinet. 2010;49:549-58 pubmed publisher
    ..A population pharmacokinetic model that included CDA genotypes as a covariate for gemcitabine and dFdU in Japanese cancer patients was successfully constructed. The model confirms the clinical importance of the CDA*3 genotype. ..
  37. Borbath I, Verbrugghe L, Lai R, Gigot J, Humblet Y, Piessevaux H, et al. Human equilibrative nucleoside transporter 1 (hENT1) expression is a potential predictive tool for response to gemcitabine in patients with advanced cholangiocarcinoma. Eur J Cancer. 2012;48:990-6 pubmed publisher
    ..The combined administration of cisplatin and gemcitabine is considered standard of care. Human equilibrative nucleoside transporter 1 (hENT1) is the major transporter responsible for gemcitabine uptake into cells...
  38. Eto K, Kawakami H, Kuwatani M, Kudo T, Abe Y, Kawahata S, et al. Human equilibrative nucleoside transporter 1 and Notch3 can predict gemcitabine effects in patients with unresectable pancreatic cancer. Br J Cancer. 2013;108:1488-94 pubmed publisher
    ..The expressions of human equilibrative nucleoside transporter 1 (hENT1), deoxycitidine kinase, ribonucleoside reductase 1, ribonucleoside reductase 2 and Notch3 ..
  39. Griffiths M, Yao S, Abidi F, Phillips S, Cass C, Young J, et al. Molecular cloning and characterization of a nitrobenzylthioinosine-insensitive (ei) equilibrative nucleoside transporter from human placenta. Biochem J. 1997;328 ( Pt 3):739-43 pubmed
    ..reported the isolation of a cDNA clone encoding a prototypic es-type transporter, hENT1 (human equilibrative nucleoside transporter 1), from human placenta...
  40. Sundaram M, Yao S, Ingram J, Berry Z, Abidi F, Cass C, et al. Topology of a human equilibrative, nitrobenzylthioinosine (NBMPR)-sensitive nucleoside transporter (hENT1) implicated in the cellular uptake of adenosine and anti-cancer drugs. J Biol Chem. 2001;276:45270-5 pubmed
    ..Sequence analyses suggest that this membrane topology is common to all mammalian, insect, nematode, protozoan, yeast, and plant members of the ENT protein family. ..
  41. Santini D, Perrone G, Vincenzi B, Lai R, Cass C, Alloni R, et al. Human equilibrative nucleoside transporter 1 (hENT1) protein is associated with short survival in resected ampullary cancer. Ann Oncol. 2008;19:724-8 pubmed publisher
    ..The human equilibrative nucleoside transporter 1 (hENT1) is a ubiquitous protein and is the major means by which gemcitabine enters human cells...
  42. Lin W, Buolamwini J. Synthesis, flow cytometric evaluation, and identification of highly potent dipyridamole analogues as equilibrative nucleoside transporter 1 inhibitors. J Med Chem. 2007;50:3906-20 pubmed
    ..The SAR indicated that diethanolamine substituted analogues were more active than monoethanolamine compounds. Also, free hydroxyl groups are not essential for activity. ..
  43. Bone D, Robillard K, Stolk M, Hammond J. Differential regulation of mouse equilibrative nucleoside transporter 1 (mENT1) splice variants by protein kinase CK2. Mol Membr Biol. 2007;24:294-303 pubmed
    ..In conclusion, inhibition of CK2 activity, or deletion of Ser(254) from mENT1, enhances transporter affinity for the inhibitor, NBMPR, and reduces the number of ENT1 proteins functioning at the level of the plasma membrane. ..
  44. Lai Y, Tse C, Unadkat J. Mitochondrial expression of the human equilibrative nucleoside transporter 1 (hENT1) results in enhanced mitochondrial toxicity of antiviral drugs. J Biol Chem. 2004;279:4490-7 pubmed
    ..To test this hypothesis, we have sought to determine whether the nucleoside transporters, human equilibrative nucleoside transporter 1 (hENT1) or human concentrative nucleoside transporter 1 (hCNT1), when stably expressed in Madin-..
  45. Chaudary N, Naydenova Z, Shuralyova I, Coe I. Hypoxia regulates the adenosine transporter, mENT1, in the murine cardiomyocyte cell line, HL-1. Cardiovasc Res. 2004;61:780-8 pubmed
    ..Cardiomyocytes may regulate mENT1 (via PKC) to modulate release and/or uptake of adenosine. However, the relationship between mENT1 mRNA levels, protein levels and functional transport is complex. ..
  46. Myers S, Goyal R, Roy J, Fairfull L, Wilson J, Ferrell R. Functional single nucleotide polymorphism haplotypes in the human equilibrative nucleoside transporter 1. Pharmacogenet Genomics. 2006;16:315-20 pubmed
    The human equilibrative nucleoside transporter 1 gene (hENT1) is the primary nucleoside transporter for cytosine arabinoside (AraC), a deoxycytidine analog used for treatment of acute leukemias and lymphomas. We screened approximately 1...
  47. Rose J, Naydenova Z, Bang A, Eguchi M, Sweeney G, Choi D, et al. Equilibrative nucleoside transporter 1 plays an essential role in cardioprotection. Am J Physiol Heart Circ Physiol. 2010;298:H771-7 pubmed publisher
  48. Giovannetti E, Del Tacca M, Mey V, Funel N, Nannizzi S, Ricci S, et al. Transcription analysis of human equilibrative nucleoside transporter-1 predicts survival in pancreas cancer patients treated with gemcitabine. Cancer Res. 2006;66:3928-35 pubmed
    ..This study suggests that the expression levels of hENT1 may allow the stratification of patients based on their likelihood of survival, thus offering a potential new tool for treatment optimization. ..
  49. Kost S, Sun C, Xiong W, Graham K, Cass C, Young J, et al. Behavioral effects of elevated expression of human equilibrative nucleoside transporter 1 in mice. Behav Brain Res. 2011;224:44-9 pubmed publisher
    ..Transgenic mice with neuronal expression of human equilibrative nucleoside transporter 1 (hENT1) have been generated (Parkinson et al., 2009 [7])...
  50. Lang T, Selner M, Young J, Cass C. Acquisition of human concentrative nucleoside transporter 2 (hcnt2) activity by gene transfer confers sensitivity to fluoropyrimidine nucleosides in drug-resistant leukemia cells. Mol Pharmacol. 2001;60:1143-52 pubmed
    ..These studies, which demonstrated hCNT2 uptake of halogenated uridine analogs, suggested that hCNT2 is an important determinant of cytotoxicity of this class of compounds in vivo. ..
  51. Osato D, Huang C, Kawamoto M, Johns S, Stryke D, Wang J, et al. Functional characterization in yeast of genetic variants in the human equilibrative nucleoside transporter, ENT1. Pharmacogenetics. 2003;13:297-301 pubmed
    ..These results, together with the observation that there are few haplotypes of ENT1, indicate that coding region variants of ENT1 do not contribute to inter-individual differences in response to nucleoside analog drugs. ..
  52. Kobayashi H, Murakami Y, Uemura K, Sudo T, Hashimoto Y, Kondo N, et al. Human equilibrative nucleoside transporter 1 expression predicts survival of advanced cholangiocarcinoma patients treated with gemcitabine-based adjuvant chemotherapy after surgical resection. Ann Surg. 2012;256:288-96 pubmed publisher
    The aim of this study was to evaluate whether intratumoral human equilibrative nucleoside transporter 1 (hENT1) expression can predict the survival of advanced cholangiocarcinoma patients treated with adjuvant gemcitabine-based ..
  53. Kawada N, Uehara H, Katayama K, Nakamura S, Takahashi H, Ohigashi H, et al. Human equilibrative nucleoside transporter 1 level does not predict prognosis in pancreatic cancer patients treated with neoadjuvant chemoradiation including gemcitabine. J Hepatobiliary Pancreat Sci. 2012;19:717-22 pubmed publisher
    Gemcitabine is a key drug for the treatment of pancreatic cancer. Human equilibrative nucleoside transporter 1 (hENT1) is a major transporter responsible for gemcitabine uptake into cells...
  54. Achiwa H, Oguri T, Sato S, Maeda H, Niimi T, Ueda R. Determinants of sensitivity and resistance to gemcitabine: the roles of human equilibrative nucleoside transporter 1 and deoxycytidine kinase in non-small cell lung cancer. Cancer Sci. 2004;95:753-7 pubmed
    ..In this study we used quantitative RT-PCR to examine the expression levels of human equilibrative nucleoside transporter 1 (hENT1) and deoxycytidine kinase (dCK) genes in non-small cell lung cancer (NSCLC) cell lines in ..
  55. Chow L, Lai R, Dabbagh L, Belch A, Young J, Cass C, et al. Analysis of human equilibrative nucleoside transporter 1 (hENT1) protein in non-Hodgkin's lymphoma by immunohistochemistry. Mod Pathol. 2005;18:558-64 pubmed
    The human equilibrative nucleoside transporter 1 (hENT1) is a member of the equilibrative nucleoside transporter family that mediates cellular entry of gemcitabine, cytarabine, and fludarabine...
  56. Hubeek I, Stam R, Peters G, Broekhuizen R, Meijerink J, van Wering E, et al. The human equilibrative nucleoside transporter 1 mediates in vitro cytarabine sensitivity in childhood acute myeloid leukaemia. Br J Cancer. 2005;93:1388-94 pubmed
    ..29; 0.04). In conclusion, decreased expression of hENT1, which transports ara-C across the cell membrane, appears to be a major factor in ara-C resistance in childhood AML. ..
  57. Westermeier F, Salomon C, Gonzalez M, Puebla C, Guzman Gutierrez E, Cifuentes F, et al. Insulin restores gestational diabetes mellitus-reduced adenosine transport involving differential expression of insulin receptor isoforms in human umbilical vein endothelium. Diabetes. 2011;60:1677-87 pubmed publisher
    ..Abnormal adenosine plasma levels, and potentially A(2A)-adenosine receptors and insulin receptor A, will play crucial roles in this phenomenon in GDM. ..
  58. Damaraju V, Elwi A, Hunter C, Carpenter P, Santos C, Barron G, et al. Localization of broadly selective equilibrative and concentrative nucleoside transporters, hENT1 and hCNT3, in human kidney. Am J Physiol Renal Physiol. 2007;293:F200-11 pubmed
  59. Gusella M, Pasini F, Bolzonella C, Meneghetti S, Barile C, Bononi A, et al. Equilibrative nucleoside transporter 1 genotype, cytidine deaminase activity and age predict gemcitabine plasma clearance in patients with solid tumours. Br J Clin Pharmacol. 2011;71:437-44 pubmed publisher
    ..77). Our results confirm the role of CDA and age on the interindividual variability of GEM CL and show the contribution of the hENT1 genotype for the first time. ..
  60. Oguri T, Achiwa H, Muramatsu H, Ozasa H, Sato S, Shimizu S, et al. The absence of human equilibrative nucleoside transporter 1 expression predicts nonresponse to gemcitabine-containing chemotherapy in non-small cell lung cancer. Cancer Lett. 2007;256:112-9 pubmed
    We report here the development of a polyclonal antibody for human equilibrative nucleoside transporter 1 (hENT1) and assess the expression of hENT1 in non-small cell lung cancer (NSCLC) patients who were treated with gemcitabine-..
  61. Nakamura J, Kohya N, Kai K, Ohtaka K, Hashiguchi K, Hiraki M, et al. Ribonucleotide reductase subunit M1 assessed by quantitative double-fluorescence immunohistochemistry predicts the efficacy of gemcitabine in biliary tract carcinoma. Int J Oncol. 2010;37:845-52 pubmed
    ..Furthermore, qDFIHC is a useful method for the assessment of RRM1 protein, in order to design a tailor-made chemotherapeutic regimen for BTC patients...
  62. Vega J, Puebla C, Vásquez R, Farias M, Alarcon J, Pastor Anglada M, et al. TGF-beta1 inhibits expression and activity of hENT1 in a nitric oxide-dependent manner in human umbilical vein endothelium. Cardiovasc Res. 2009;82:458-67 pubmed publisher
    ..These findings comprise physiological mechanisms that could be important in diseases where TGF-beta1 plasma level is increased as in gestational diabetic mothers or patients with diabetes mellitus. ..
  63. Parkinson F, Xiong W, Zamzow C, Chestley T, Mizuno T, Duckworth M. Transgenic expression of human equilibrative nucleoside transporter 1 in mouse neurons. J Neurochem. 2009;109:562-72 pubmed publisher
    ..Instead, hENT1 expression affects dynamic changes in endogenous adenosine levels, as revealed by altered behavioral responses to drugs that affect adenosine receptor signalling. ..
  64. Jin G, Matsushita H, Asai S, Tsukamoto H, Ono R, Nosaka T, et al. FLT3-ITD induces ara-C resistance in myeloid leukemic cells through the repression of the ENT1 expression. Biochem Biophys Res Commun. 2009;390:1001-6 pubmed publisher
    ..cytosine arabinoside (ara-C), an essential agent for AML, accompanied by the downregulation of equilibrative nucleoside transporter 1 (ENT1), a transporter responsible for the cellular uptake of ara-C...