Article
The prokaryote ligand-gated ion channel ELIC captured in a pore blocker-bound conformation by the Alzheimer's disease drug memantine.
Structure (London, England : 1993) - 7 Oct 2014
Ulens Chris, Spurny Radovan, Thompson Andrew J, Alqazzaz Mona, Debaveye Sarah, Han Lu, Price Kerry, Villalgordo Jose M, Tresadern Gary, Lynch Joseph W, Lummis Sarah C R
Abstract excerpt
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...
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