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4l17

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{{STRUCTURE_4l17| PDB=4l17 | SCENE= }}
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==GluA2-L483Y-A665C ligand-binding domain in complex with the antagonist DNQX==
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===GluA2-L483Y-A665C ligand-binding domain in complex with the antagonist DNQX===
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<StructureSection load='4l17' size='340' side='right' caption='[[4l17]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
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{{ABSTRACT_PUBMED_23931998}}
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4l17]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4L17 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4L17 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=DNQ:6,7-DINITROQUINOXALINE-2,3-DIONE'>DNQ</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Gria2, Glur2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus])</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=4l17 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4l17 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4l17 RCSB], [http://www.ebi.ac.uk/pdbsum/4l17 PDBsum]</span></td></tr>
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</table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Ionotropic glutamate receptors (iGluRs) transduce the chemical signal of neurotransmitter release into membrane depolarization at excitatory synapses in the brain. The opening of the transmembrane ion channel of these ligand-gated receptors is driven by conformational transitions that are induced by the association of glutamate molecules to the ligand-binding domains (LBDs). Here, we describe the crystal structure of a GluA2 LBD tetramer in a configuration that involves an approximately 30 degrees rotation of the LBD dimers relative to the crystal structure of the full-length receptor. The configuration is stabilized by an engineered disulfide crosslink. Biochemical and electrophysiological studies on full-length receptors incorporating either this crosslink or an engineered metal bridge show that this LBD configuration corresponds to an intermediate state of receptor activation. GluA2 activation therefore involves a combination of both intra-LBD (cleft closure) and inter-LBD dimer conformational transitions. Overall, these results provide a comprehensive structural characterization of an iGluR intermediate state.
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==Function==
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A conformational intermediate in glutamate receptor activation.,Lau AY, Salazar H, Blachowicz L, Ghisi V, Plested AJ, Roux B Neuron. 2013 Aug 7;79(3):492-503. doi: 10.1016/j.neuron.2013.06.003. PMID:23931998<ref>PMID:23931998</ref>
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[[http://www.uniprot.org/uniprot/GRIA2_RAT GRIA2_RAT]] Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate.<ref>PMID:9351977</ref> <ref>PMID:19265014</ref> <ref>PMID:21172611</ref> <ref>PMID:12501192</ref> <ref>PMID:12015593</ref> <ref>PMID:12872125</ref> <ref>PMID:12730367</ref> <ref>PMID:16192394</ref> <ref>PMID:15591246</ref> <ref>PMID:17018279</ref> <ref>PMID:16483599</ref> <ref>PMID:19946266</ref> <ref>PMID:21317873</ref> <ref>PMID:21846932</ref>
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==About this Structure==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[4l17]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4L17 OCA].
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</div>
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==Reference==
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==See Also==
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<ref group="xtra">PMID:023931998</ref><references group="xtra"/><references/>
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*[[Ionotropic Glutamate Receptors|Ionotropic Glutamate Receptors]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Blachowicz, L.]]
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[[Category: Blachowicz, L]]
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[[Category: Lau, A Y.]]
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[[Category: Lau, A Y]]
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[[Category: Roux, B.]]
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[[Category: Roux, B]]
[[Category: Ion channel]]
[[Category: Ion channel]]
[[Category: Membrane]]
[[Category: Membrane]]
[[Category: Neuroreceptor]]
[[Category: Neuroreceptor]]
[[Category: Transport protein]]
[[Category: Transport protein]]

Revision as of 14:27, 21 December 2014

GluA2-L483Y-A665C ligand-binding domain in complex with the antagonist DNQX

4l17, resolution 2.80Å

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