A second extracellular site is required for norepinephrine transport by the human norepinephrine transporter.

@article{Wang2012ASE,
  title={A second extracellular site is required for norepinephrine transport by the human norepinephrine transporter.},
  author={C A Wang and Nausad H. Shaikh and S. Naga Ramu and Richard J Lewis},
  journal={Molecular pharmacology},
  year={2012},
  volume={82 5},
  pages={898-909}
}
The human norepinephrine transporter (NET) is implicated in many neurological disorders and is a target of tricyclic antidepressants and nisoxetine (NX). We used molecular docking simulations to guide the identification of residues likely to affect substrate transport and ligand interactions at NET. Mutations to alanine identified a hydrophobic pocket in the extracellular cavity of NET, comprising residues Thr80, Phe317, and Tyr317, which was critical for efficient norepinephrine (NE) transport… CONTINUE READING