Articles with "ent1" as a keyword



Numerical analysis of apparent decitabine uptake in HCT116 cells: Incorporation of a bidirectional first-order kinetic parameter for ENT1 transport and Michaelis-Menten parameters for subsequent phosphorylation.

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Published in 2019 at "Drug metabolism and pharmacokinetics"

DOI: 10.1016/j.dmpk.2019.10.002

Abstract: Decitabine (DAC), a DNA methylation inhibitor, is transported into cancer cells mainly via equilibrative nucleoside transporter 1 (ENT1) and subsequently phosphorylated by deoxycytidine kinase (dCK). We previously reported that apparent DAC uptake into cells may be… read more here.

Keywords: michaelis menten; hct116 cells; menten parameters; subsequent phosphorylation ... See more keywords

Targeting ENT1 and adenosine tone for the treatment of Huntington's disease

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Published in 2017 at "Human Molecular Genetics"

DOI: 10.1093/hmg/ddw402

Abstract: &NA; Huntington's disease (HD) is caused by an abnormal CAG expansion in the exon 1 of huntingtin gene. The treatment of HD is an unmet medical need. Given the important role of adenosine in modulating… read more here.

Keywords: adenosine tone; ent1; adenosine; huntington disease ... See more keywords

Development of a Novel HEK293 Cell Model Lacking SLC29A1 to Study the Pharmacology of Endogenous SLC29A2-Encoded Equilibrative Nucleoside Transporter Subtype 2

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Published in 2024 at "Drug Metabolism and Disposition"

DOI: 10.1124/dmd.124.001814

Abstract: Equilibrative nucleoside transporters (ENTs) mediate the transmembrane flux of endogenous nucleosides and nucleoside analogs used clinically. The predominant subtype, ENT1, has been well characterized. However, the other subtype, ENT2, has been less well characterized in… read more here.

Keywords: ent1; pharmacology; ent2; cell ... See more keywords