Thermodynamics and kinetics of inhibitor binding to human equilibrative nucleoside transporter subtype-1.

@article{Rehan2015ThermodynamicsAK,
  title={Thermodynamics and kinetics of inhibitor binding to human equilibrative nucleoside transporter subtype-1.},
  author={Shahid Rehan and Yashwanth Ashok and Rahul Nanekar and Veli-Pekka Jaakola},
  journal={Biochemical pharmacology},
  year={2015},
  volume={98 4},
  pages={681-9}
}
Many nucleoside transport inhibitors are in clinical use as anti-cancer, vasodilator and cardioprotective drugs. However, little is known about the binding energetics of these inhibitors to nucleoside transporters (NTs) due to their low endogenous expression levels and difficulties in the biophysical characterization of purified protein with ligands. Here, we present kinetics and thermodynamic analyses of inhibitor binding to the human equilibrative nucleoside transporter-1 (hENT1), also known… CONTINUE READING
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