1995
DOI: 10.1038/bjc.1995.437
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Modulation of the equilibrative nucleoside transporter by inhibitors of DNA synthesis

Abstract: In contrast, cytosine arabinoside (ara-C) and aphidicolin, which directly inhibit DNA synthesis, produced no significant increase in es expression. Thymidine (TdR), which is an allosteric inhibitor of ribonucleotide reductase that depletes dATP, dCTP and dGTP pools while repleting the dTTP pool, had no significant effect on es expression. These data suggest that surface expression of the es nucleoside transporter is regulated by a mechanism which is sensitive to the supply of deoxynucleotides. Because 5-FU (wh… Show more

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Cited by 40 publications
(22 citation statements)
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“…In particular, gemcitabine is most efficiently transported by hENT1, and activity of this protein is considered to be a possible determinant of drug efficacy (Mackey et al, 1998). Because TS inhibitors upregulate hENT1 and increase gemcitabine sensitivity by depleting intracellular nucleotide pools (Pressacco et al, 1995;Rauchwerger et al, 2000), the present study analyzed the modulation of hENT1 expression by pemetrexed and demonstrated a significant up-regulation of this carrier, potentially facilitating gemcitabine cytotoxicity.…”
Section: Discussionmentioning
confidence: 99%
“…In particular, gemcitabine is most efficiently transported by hENT1, and activity of this protein is considered to be a possible determinant of drug efficacy (Mackey et al, 1998). Because TS inhibitors upregulate hENT1 and increase gemcitabine sensitivity by depleting intracellular nucleotide pools (Pressacco et al, 1995;Rauchwerger et al, 2000), the present study analyzed the modulation of hENT1 expression by pemetrexed and demonstrated a significant up-regulation of this carrier, potentially facilitating gemcitabine cytotoxicity.…”
Section: Discussionmentioning
confidence: 99%
“…However, when asynchronous cells are treated, cells that are in S phase at the time of aphidicolin addition are arrested within S phase (21). In such cells, deoxyribonucleotide precursor levels are apparently preserved (42), and thus cells in S phase at the time of arrest may be able to support reverse transcription. Therefore, the ability of ASV to transduce aphidicolin-arrested cells (Fig.…”
Section: Discussionmentioning
confidence: 99%
“…Twenty-four hours after seeding in 6-well plates at 3x10 5 Flow cytometric analysis. Cells treated with vehicle or etoposide for 24 h were trypsinized, fixed in 70% ethanol, stained with propidium iodide, and subjected to flow cytometry (Becton Dickinson, San Jose, CA).…”
Section: Ent1 Activity In the Plasmamentioning
confidence: 99%