4twd: Difference between revisions
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==X-ray structure of a pentameric ligand gated ion channel from Erwinia chrysanthemi (ELIC) in complex with memantine== | ==X-ray structure of a pentameric ligand gated ion channel from Erwinia chrysanthemi (ELIC) in complex with memantine== | ||
<StructureSection load='4twd' size='340' side='right' caption='[[4twd]], [[Resolution|resolution]] 3.20Å' scene=''> | <StructureSection load='4twd' size='340' side='right' caption='[[4twd]], [[Resolution|resolution]] 3.20Å' scene=''> | ||
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<table><tr><td colspan='2'>[[4twd]] is a 10 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4TWD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4TWD FirstGlance]. <br> | <table><tr><td colspan='2'>[[4twd]] is a 10 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4TWD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4TWD FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=377:MEMANTINE'>377</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=377:MEMANTINE'>377</scene></td></tr> | ||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4twd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4twd OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4twd RCSB], [http://www.ebi.ac.uk/pdbsum/4twd PDBsum]</span></td></tr> | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4twd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4twd OCA], [http://pdbe.org/4twd PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4twd RCSB], [http://www.ebi.ac.uk/pdbsum/4twd PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4twd ProSAT]</span></td></tr> | ||
</table> | </table> | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
<div class="pdbe-citations 4twd" style="background-color:#fffaf0;"></div> | |||
==See Also== | |||
*[[Ion channels|Ion channels]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
Revision as of 14:46, 11 August 2016
X-ray structure of a pentameric ligand gated ion channel from Erwinia chrysanthemi (ELIC) in complex with memantineX-ray structure of a pentameric ligand gated ion channel from Erwinia chrysanthemi (ELIC) in complex with memantine
Structural highlights
Publication Abstract from PubMedPentameric 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-memantine, reveal that the ligand is localized at the extracellular entryway of the channel pore, and the pore is in a more closed conformation than wild-type ELIC in both the presence and absence of memantine. However, using voltage clamp fluorometry we observe fluorescence changes in opposite directions during channel activation and pore block, revealing an additional conformational transition not apparent from the crystal structures. These results have important implications for drugs such as memantine, which block channel pores. The Prokaryote Ligand-Gated Ion Channel ELIC Captured in a Pore Blocker-Bound Conformation by the Alzheimer's Disease Drug Memantine.,Ulens C, Spurny R, Thompson AJ, Alqazzaz M, Debaveye S, Han L, Price K, Villalgordo JM, Tresadern G, Lynch JW, Lummis SC Structure. 2014 Sep 3. pii: S0969-2126(14)00244-5. doi:, 10.1016/j.str.2014.07.013. PMID:25199693[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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