Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain.

@article{Abrahamsen2013AllostericMO,
  title={Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain.},
  author={Bjarke Abrahamsen and Nicole Schneider and Mette N. Erichsen and Tri H V Huynh and Christoph Fahlke and Lennart Bunch and Anders A Jensen},
  journal={The Journal of neuroscience : the official journal of the Society for Neuroscience},
  year={2013},
  volume={33 3},
  pages={1068-87}
}
In the present study, the mechanism of action and molecular basis for the activity of the first class of selective inhibitors of the human excitatory amino acid transporter subtype 1 (EAAT1) and its rodent ortholog GLAST are elucidated. The previously reported specificity of UCPH-101 and UCPH-102 for EAAT1 over EAAT2 and EAAT3 is demonstrated to extend to… CONTINUE READING