The prokaryote ligand-gated ion channel ELIC captured in a pore blocker-bound conformation by the Alzheimer's disease drug memantine.

@article{Ulens2014ThePL,
  title={The prokaryote ligand-gated ion channel ELIC captured in a pore blocker-bound conformation by the Alzheimer's disease drug memantine.},
  author={Chris Ulens and Radovan Spurny and Andrew J Thompson and Mona A Alqazzaz and Sarah Debaveye and Lu Han and Kerry. L. Price and Jose Manuel Villalgordo and Gary Tresadern and Joseph W Lynch and Sarah C. R. Lummis},
  journal={Structure},
  year={2014},
  volume={22 10},
  pages={1399-407}
}
Pentameric ligand-gated ion channels (pLGIC) catalyze the selective transfer of ions across the cell membrane in response to a specific neurotransmitter. A variety of chemically diverse molecules, including the Alzheimer's drug memantine, block ion conduction at vertebrate pLGICs by plugging the channel pore. We show that memantine has similar potency in ELIC, a prokaryotic pLGIC, when it contains an F16'S pore mutation. X-ray crystal structures, using both memantine and its derivative, Br… CONTINUE READING
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