4hfe
From Proteopedia
(Difference between revisions)
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| - | + | ==The GLIC pentameric Ligand-Gated Ion Channel F14'A ethanol-sensitive mutant complexed to ethanol== | |
| - | + | <StructureSection load='4hfe' size='340' side='right' caption='[[4hfe]], [[Resolution|resolution]] 2.80Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[4hfe]] is a 5 chain structure with sequence from [http://en.wikipedia.org/wiki/Gloeobacter_violaceus_pcc_7421 Gloeobacter violaceus pcc 7421]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4HFE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4HFE FirstGlance]. <br> | |
| - | ==Function== | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=EOH:ETHANOL'>EOH</scene>, <scene name='pdbligand=LMT:DODECYL-BETA-D-MALTOSIDE'>LMT</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=PLC:DIUNDECYL+PHOSPHATIDYL+CHOLINE'>PLC</scene>, <scene name='pdbligand=UNL:UNKNOWN+LIGAND'>UNL</scene></td></tr> |
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4hfb|4hfb]], [[4hfc|4hfc]], [[4hfd|4hfd]], [[4hfh|4hfh]]</td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">glvI, glr4197 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=251221 Gloeobacter violaceus PCC 7421])</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=4hfe FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4hfe OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4hfe RCSB], [http://www.ebi.ac.uk/pdbsum/4hfe PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
[[http://www.uniprot.org/uniprot/GLIC_GLOVI GLIC_GLOVI]] Cationic channel with similar permeabilities for Na(+) and K(+), that is activated by an increase of the proton concentration on the extracellular side. Displays no permeability for chloride ions. Shows slow kinetics of activation, no desensitization and a single channel conductance of 8 pS. Might contribute to adaptation to external pH change.<ref>PMID:17167423</ref> | [[http://www.uniprot.org/uniprot/GLIC_GLOVI GLIC_GLOVI]] Cationic channel with similar permeabilities for Na(+) and K(+), that is activated by an increase of the proton concentration on the extracellular side. Displays no permeability for chloride ions. Shows slow kinetics of activation, no desensitization and a single channel conductance of 8 pS. Might contribute to adaptation to external pH change.<ref>PMID:17167423</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Ethanol alters nerve signalling by interacting with proteins in the central nervous system, particularly pentameric ligand-gated ion channels. A recent series of mutagenesis experiments on Gloeobacter violaceus ligand-gated ion channel, a prokaryotic member of this family, identified a single-site variant that is potentiated by pharmacologically relevant concentrations of ethanol. Here we determine crystal structures of the ethanol-sensitized variant in the absence and presence of ethanol and related modulators, which bind in a transmembrane cavity between channel subunits and may stabilize the open form of the channel. Structural and mutagenesis studies defined overlapping mechanisms of potentiation by alcohols and anaesthetics via the inter-subunit cavity. Furthermore, homology modelling show this cavity to be conserved in human ethanol-sensitive glycine and GABA(A) receptors, and to involve residues previously shown to influence alcohol and anaesthetic action on these proteins. These results suggest a common structural basis for ethanol potentiation of an important class of targets for neurological actions of ethanol. | ||
| - | + | Structural basis for potentiation by alcohols and anaesthetics in a ligand-gated ion channel.,Sauguet L, Howard RJ, Malherbe L, Lee US, Corringer PJ, Harris RA, Delarue M Nat Commun. 2013;4:1697. doi: 10.1038/ncomms2682. PMID:23591864<ref>PMID:23591864</ref> | |
| - | + | ||
| - | == | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> |
| - | + | </div> | |
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
[[Category: Gloeobacter violaceus pcc 7421]] | [[Category: Gloeobacter violaceus pcc 7421]] | ||
| - | [[Category: Corringer, P J | + | [[Category: Corringer, P J]] |
| - | [[Category: Delarue, M | + | [[Category: Delarue, M]] |
| - | [[Category: Harris, R A | + | [[Category: Harris, R A]] |
| - | [[Category: Howard, R J | + | [[Category: Howard, R J]] |
| - | [[Category: Lee, U S | + | [[Category: Lee, U S]] |
| - | [[Category: Malherbe, L | + | [[Category: Malherbe, L]] |
| - | [[Category: Sauguet, L | + | [[Category: Sauguet, L]] |
[[Category: Ion-channel]] | [[Category: Ion-channel]] | ||
[[Category: Membrane protein]] | [[Category: Membrane protein]] | ||
[[Category: Pentameric transmembrane channel]] | [[Category: Pentameric transmembrane channel]] | ||
[[Category: Transport protein]] | [[Category: Transport protein]] | ||
Revision as of 20:29, 24 December 2014
The GLIC pentameric Ligand-Gated Ion Channel F14'A ethanol-sensitive mutant complexed to ethanol
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