4f8h

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==X-ray Structure of the Anesthetic Ketamine Bound to the GLIC Pentameric Ligand-gated Ion Channel==
==X-ray Structure of the Anesthetic Ketamine Bound to the GLIC Pentameric Ligand-gated Ion Channel==
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<StructureSection load='4f8h' size='340' side='right' caption='[[4f8h]], [[Resolution|resolution]] 2.99&Aring;' scene=''>
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<StructureSection load='4f8h' size='340' side='right'caption='[[4f8h]], [[Resolution|resolution]] 2.99&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4f8h]] is a 5 chain structure with sequence from [http://en.wikipedia.org/wiki/Gloeobacter_violaceus Gloeobacter violaceus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4F8H OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4F8H FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4f8h]] is a 5 chain structure with sequence from [https://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=4F8H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4F8H FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LMD:TETRADECYL+4-O-ALPHA-D-GLUCOPYRANOSYL-BETA-D-GLUCOPYRANOSIDE'>LMD</scene>, <scene name='pdbligand=PC1:1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>PC1</scene>, <scene name='pdbligand=RKE:(R)-KETAMINE'>RKE</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.99&#8491;</td></tr>
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<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=33072 Gloeobacter violaceus])</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=LMD:TETRADECYL+4-O-ALPHA-D-GLUCOPYRANOSYL-BETA-D-GLUCOPYRANOSIDE'>LMD</scene>, <scene name='pdbligand=PC1:1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>PC1</scene>, <scene name='pdbligand=RKE:(R)-KETAMINE'>RKE</scene></td></tr>
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<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=4f8h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4f8h OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4f8h RCSB], [http://www.ebi.ac.uk/pdbsum/4f8h PDBsum]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4f8h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4f8h OCA], [https://pdbe.org/4f8h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4f8h RCSB], [https://www.ebi.ac.uk/pdbsum/4f8h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4f8h ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[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>
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[https://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>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Pentameric ligand-gated ion channels (pLGICs) are targets of general anesthetics, but a structural understanding of anesthetic action on pLGICs remains elusive. GLIC, a prokaryotic pLGIC, can be inhibited by anesthetics, including ketamine. The ketamine concentration leading to half-maximal inhibition of GLIC (58 muM) is comparable to that on neuronal nicotinic acetylcholine receptors. A 2.99 A resolution X-ray structure of GLIC bound with ketamine revealed ketamine binding to an intersubunit cavity that partially overlaps with the homologous antagonist-binding site in pLGICs. The functional relevance of the identified ketamine site was highlighted by profound changes in GLIC activation upon cysteine substitution of the cavity-lining residue N152. The relevance is also evidenced by changes in ketamine inhibition upon the subsequent chemical labeling of N152C. The results provide structural insight into the molecular recognition of ketamine and are valuable for understanding the actions of anesthetics and other allosteric modulators on pLGICs.
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Structure of the Pentameric Ligand-Gated Ion Channel GLIC Bound with Anesthetic Ketamine.,Pan J, Chen Q, Willenbring D, Mowrey D, Kong XP, Cohen A, Divito CB, Xu Y, Tang P Structure. 2012 Sep 5;20(9):1463-9. PMID:22958642<ref>PMID:22958642</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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==See Also==
==See Also==
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*[[Ion channels|Ion channels]]
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*[[Ion channels 3D structures|Ion channels 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Gloeobacter violaceus]]
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[[Category: Gloeobacter violaceus PCC 7421]]
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[[Category: Chen, Q]]
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[[Category: Large Structures]]
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[[Category: Cohen, A]]
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[[Category: Chen Q]]
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[[Category: Kong, X P]]
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[[Category: Cohen A]]
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[[Category: Pan, J J]]
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[[Category: Kong XP]]
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[[Category: Tang, P]]
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[[Category: Pan JJ]]
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[[Category: Willenbring, D]]
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[[Category: Tang P]]
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[[Category: Xu, Y]]
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[[Category: Willenbring D]]
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[[Category: Anesthetic]]
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[[Category: Xu Y]]
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[[Category: Ion channel]]
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[[Category: Ketamine]]
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[[Category: Pentameric ligand-gated ion channel]]
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[[Category: Transport protein]]
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Current revision

X-ray Structure of the Anesthetic Ketamine Bound to the GLIC Pentameric Ligand-gated Ion Channel

PDB ID 4f8h

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