Chloride channels of glycine and GABA receptors with blockers: Monte Carlo minimization and structure-activity relationships.

@article{Zhorov2000ChlorideCO,
  title={Chloride channels of glycine and GABA receptors with blockers: Monte Carlo minimization and structure-activity relationships.},
  author={Boris S. Zhorov and Piotr D Bregestovski},
  journal={Biophysical journal},
  year={2000},
  volume={78 4},
  pages={1786-803}
}
GABA and glycine receptors (GlyRs) are pentameric ligand-gated ion channels that respond to the inhibitory neurotransmitters by opening a chloride-selective central pore lined with five M2 segments homologous to those of alpha(1) GlyR/ ARVG(2')LGIT(6')TVLTMTTQSSGSR. The activity of cyanotriphenylborate (CTB) and picrotoxinin (PTX), the best-studied blockers of the Cl(-) pores, depends essentially on the subunit composition of the receptors, in particular, on residues in positions 2' and 6' that… CONTINUE READING