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3bki

From Proteopedia

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[[Image:3bki.png|left|200px]]
 
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{{STRUCTURE_3bki| PDB=3bki | SCENE= }}
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==Crystal Structure of the GluR2 ligand binding core (S1S2J) in complex with FQX at 1.87 Angstroms==
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<StructureSection load='3bki' size='340' side='right'caption='[[3bki]], [[Resolution|resolution]] 1.87&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3bki]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Buffalo_rat Buffalo rat]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3BKI OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3BKI FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=FQX:[1,2,5]OXADIAZOLO[3,4-G]QUINOXALINE-6,7(5H,8H)-DIONE+1-OXIDE'>FQX</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[3bkg|3bkg]]</div></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Gria2, Glur2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat])</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=3bki FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3bki OCA], [https://pdbe.org/3bki PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3bki RCSB], [https://www.ebi.ac.uk/pdbsum/3bki PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3bki ProSAT]</span></td></tr>
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</table>
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== Function ==
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[[https://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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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/bk/3bki_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3bki ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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AMPA receptors mediate fast excitatory synaptic transmission and are essential for synaptic plasticity. ANQX, a photoreactive AMPA receptor antagonist, is an important biological probe used to irreversibly inactivate AMPA receptors. Here, using X-ray crystallography and mass spectroscopy, we report that ANQX forms two major products in the presence of the GluR2 AMPAR ligand-binding core (S1S2J). Upon photostimulation, ANQX reacts intramolecularly to form FQX or intermolecularly to form a covalent adduct with Glu705.
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===Crystal Structure of the GluR2 ligand binding core (S1S2J) in complex with FQX at 1.87 Angstroms===
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6-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) Forms an Irreversible Bond To the Active Site of the GluR2 AMPA Receptor.,Cruz LA, Estebanez-Perpina E, Pfaff S, Borngraeber S, Bao N, Blethrow J, Fletterick RJ, England PM J Med Chem. 2008 Aug 28. PMID:18754610<ref>PMID:18754610</ref>
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{{ABSTRACT_PUBMED_18754610}}
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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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==About this Structure==
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<div class="pdbe-citations 3bki" style="background-color:#fffaf0;"></div>
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[[3bki]] 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=3BKI OCA].
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==See Also==
==See Also==
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*[[Ionotropic Glutamate Receptors|Ionotropic Glutamate Receptors]]
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*[[Glutamate receptor 3D structures|Glutamate receptor 3D structures]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:018754610</ref><references group="xtra"/>
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__TOC__
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[[Category: Rattus norvegicus]]
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</StructureSection>
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[[Category: Bao, N.]]
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[[Category: Buffalo rat]]
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[[Category: Borngraeber, S.]]
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[[Category: Large Structures]]
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[[Category: Cruz, L.]]
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[[Category: Bao, N]]
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[[Category: England, P.]]
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[[Category: Borngraeber, S]]
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[[Category: Estebanez-Perpina, E.]]
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[[Category: Cruz, L]]
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[[Category: Fletterick, R.]]
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[[Category: England, P]]
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[[Category: Pfaff, S.]]
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[[Category: Estebanez-Perpina, E]]
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[[Category: Fletterick, R]]
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[[Category: Pfaff, S]]
[[Category: 3-dione]]
[[Category: 3-dione]]
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[[Category: Alternative splicing]]
[[Category: Ampa receptor]]
[[Category: Ampa receptor]]
[[Category: Anqx]]
[[Category: Anqx]]

Current revision

Crystal Structure of the GluR2 ligand binding core (S1S2J) in complex with FQX at 1.87 Angstroms

PDB ID 3bki

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