Structural basis of open channel block in a prokaryotic pentameric ligand-gated ion channel

@article{Hilf2010StructuralBO,
  title={Structural basis of open channel block in a prokaryotic pentameric ligand-gated ion channel},
  author={Ricarda J. C. Hilf and Carlo Bertozzi and Iwan Zimmermann and Alwin Reiter and Dirk Trauner and Raimund Dutzler},
  journal={Nature Structural &Molecular Biology},
  year={2010},
  volume={17},
  pages={1330-1336}
}
The flow of ions through cation-selective members of the pentameric ligand-gated ion channel family is inhibited by a structurally diverse class of molecules that bind to the transmembrane pore in the open state of the protein. To obtain insight into the mechanism of channel block, we have investigated the binding of positively charged inhibitors to the open channel of the bacterial homolog GLIC by using X-ray crystallography and electrophysiology. Our studies reveal the location of two regions… CONTINUE READING

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