Transport of lamivudine [(-)-beta-L-2',3'-dideoxy-3'-thiacytidine] and high-affinity interaction of nucleoside reverse transcriptase inhibitors with human organic cation transporters 1, 2, and 3.

@article{Minuesa2009TransportOL,
  title={Transport of lamivudine [(-)-beta-L-2',3'-dideoxy-3'-thiacytidine] and high-affinity interaction of nucleoside reverse transcriptase inhibitors with human organic cation transporters 1, 2, and 3.},
  author={Gerard Minuesa and Christopher Volk and M{\'i}riam Molina-Arcas and Valentin Gorboulev and Itziar Erkizia and Petra A. Arndt and Bonaventura Clotet and Marçal Pastor-Anglada and Hermann Koepsell and Javier Martinez-Picado},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2009},
  volume={329 1},
  pages={252-61}
}
Nucleoside reverse transcriptase inhibitors (NRTIs) need to enter cells to act against the HIV-1. Human organic cation transporters (hOCT1-3) are expressed and active in CD4+ T cells, the main target of HIV-1, and have been associated with antiviral uptake in different tissues. In this study, we examined whether NRTIs interact and are substrates of hOCT in cells stably expressing these transporters. Using [(3)H]N-methyl-4-phenylpyridinium, we found a high-affinity interaction among abacavir… CONTINUE READING
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