Charge and geometry of residues in the loop 2 β hairpin differentially affect agonist and ethanol sensitivity in glycine receptors.

@article{Perkins2012ChargeAG,
  title={Charge and geometry of residues in the loop 2 β hairpin differentially affect agonist and ethanol sensitivity in glycine receptors.},
  author={Daya I Perkins and James R. Trudell and Liana Asatryan and Daryl L Davies and Ronald L. Alkana},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2012},
  volume={341 2},
  pages={543-51}
}
Recent studies highlighted the importance of loop 2 of α1 glycine receptors (GlyRs) in the propagation of ligand-binding energy to the channel gate. Mutations that changed polarity at position 52 in the β hairpin of loop 2 significantly affected sensitivity to ethanol. The present study extends the investigation to charged residues. We found that substituting alanine with the negative glutamate at position 52 (A52E) significantly left-shifted the glycine concentration response curve and… CONTINUE READING