3o29

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[[Image:3o29.png|left|200px]]
 
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{{STRUCTURE_3o29| PDB=3o29 | SCENE= }}
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==Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator==
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<StructureSection load='3o29' size='340' side='right'caption='[[3o29]], [[Resolution|resolution]] 2.02&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3o29]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3O29 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3O29 FirstGlance]. <br>
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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]] 2.02&#8491;</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=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=O29:N-[2-(DIMETHYLAMINO)ETHYL]-2-({[3-(TRIFLUOROMETHYL)-4,5,6,7-TETRAHYDRO-1H-INDAZOL-1-YL]ACETYL}AMINO)-4,5,6,7-TETRAHYDRO-1-BENZOTHIOPHENE-3-CARBOXAMIDE'>O29</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></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=3o29 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3o29 OCA], [https://pdbe.org/3o29 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3o29 RCSB], [https://www.ebi.ac.uk/pdbsum/3o29 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3o29 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/o2/3o29_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.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=3o29 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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Starting from an HTS derived hit 1, application of biostructural data facilitated rapid optimization to lead 22, a novel AMPA receptor modulator. This is the first demonstration of how structure based drug design can be exploited in an optimization program for a glutamate receptor.
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===Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator===
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A novel series of positive modulators of the AMPA receptor: Discovery and structure based hit-to-lead studies.,Jamieson C, Basten S, Campbell RA, Cumming IA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Maclean JK, Moir EM, Morrow JA, Papakosta M, Rankovic Z, Smith L Bioorg Med Chem Lett. 2010 Oct 1;20(19):5753-6. Epub 2010 Aug 13. PMID:20805031<ref>PMID:20805031</ref>
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{{ABSTRACT_PUBMED_20805031}}
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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 3o29" style="background-color:#fffaf0;"></div>
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[[3o29]] is a 1 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=3O29 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:020805031</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
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[[Category: Large Structures]]
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Basten, S.]]
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[[Category: Basten S]]
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[[Category: Campbell, R A.]]
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[[Category: Campbell RA]]
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[[Category: Cumming, I A.]]
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[[Category: Cumming IA]]
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[[Category: Gillen, K J.]]
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[[Category: Gillen KJ]]
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[[Category: Gillespie, J.]]
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[[Category: Gillespie J]]
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[[Category: Jamieson, C.]]
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[[Category: Jamieson C]]
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[[Category: Kazemier, B.]]
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[[Category: Kazemier B]]
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[[Category: Kiczun, M.]]
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[[Category: Kiczun M]]
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[[Category: Lamont, Y.]]
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[[Category: Lamont Y]]
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[[Category: Lyons, A J.]]
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[[Category: Lyons AJ]]
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[[Category: Maclean, J K.F.]]
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[[Category: Maclean JKF]]
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[[Category: Moir, E M.]]
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[[Category: Moir EM]]
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[[Category: Morrow, J A.]]
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[[Category: Morrow JA]]
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[[Category: Papakosta, M.]]
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[[Category: Papakosta M]]
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[[Category: Rankovic, Z.]]
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[[Category: Rankovic Z]]
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[[Category: Smith, L.]]
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[[Category: Smith L]]
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[[Category: Chimera protein]]
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[[Category: Fusion protein]]
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[[Category: Membrane protein]]
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[[Category: Transport protein]]
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Current revision

Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator

PDB ID 3o29

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