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3o2a

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{{Seed}}
 
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[[Image:3o2a.png|left|200px]]
 
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<!--
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==Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator==
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The line below this paragraph, containing "STRUCTURE_3o2a", creates the "Structure Box" on the page.
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<StructureSection load='3o2a' size='340' side='right' caption='[[3o2a]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3o2a]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Buffalo_rat Buffalo rat]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3O2A OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3O2A FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=O30:N-(3-AMINOPROPYL)-2-({[3-(TRIFLUOROMETHYL)-4,5,6,7-TETRAHYDRO-1H-INDAZOL-1-YL]ACETYL}AMINO)-4,5,6,7-TETRAHYDRO-1-BENZOTHIOPHENE-3-CARBOXAMIDE'>O30</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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-->
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3o28|3o28]], [[3o29|3o29]], [[3o6g|3o6g]], [[3o6h|3o6h]], [[3o6i|3o6i]], [[3pmv|3pmv]], [[3pmw|3pmw]], [[3pmx|3pmx]]</td></tr>
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{{STRUCTURE_3o2a| PDB=3o2a | SCENE= }}
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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 Buffalo rat])</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=3o2a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3o2a OCA], [http://pdbe.org/3o2a PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3o2a RCSB], [http://www.ebi.ac.uk/pdbsum/3o2a PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3o2a ProSAT]</span></td></tr>
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</table>
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== Function ==
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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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== 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/o2/3o2a_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=3o2a 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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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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<div class="pdbe-citations 3o2a" style="background-color:#fffaf0;"></div>
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<!--
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_20805031}}, adds the Publication Abstract to the page
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*[[Ionotropic Glutamate Receptors|Ionotropic Glutamate Receptors]]
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(as it appears on PubMed at http://www.pubmed.gov), where 20805031 is the PubMed ID number.
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== References ==
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-->
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<references/>
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{{ABSTRACT_PUBMED_20805031}}
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__TOC__
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</StructureSection>
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==About this Structure==
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[[Category: Buffalo rat]]
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3O2A is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus,_rattus_norvegicus Rattus norvegicus, rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3O2A OCA].
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[[Category: Basten, S]]
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[[Category: Campbell, R A]]
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==Reference==
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[[Category: Cumming, I A]]
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<ref group="xtra">PMID:20805031</ref><references group="xtra"/>
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[[Category: Gillen, K J]]
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[[Category: Rattus norvegicus, rattus norvegicus]]
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[[Category: Gillespie, J]]
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[[Category: Basten, S.]]
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[[Category: Jamieson, C]]
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[[Category: Campbell, R A.]]
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[[Category: Kazemier, B]]
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[[Category: Cumming, I A.]]
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[[Category: Kiczun, M]]
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[[Category: Gillen, K J.]]
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[[Category: Lamont, Y]]
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[[Category: Gillespie, J.]]
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[[Category: Lyons, A J]]
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[[Category: Jamieson, C.]]
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[[Category: Maclean, J K.F]]
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[[Category: Kazemier, B.]]
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[[Category: Moir, E M]]
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[[Category: Kiczun, M.]]
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[[Category: Morrow, J A]]
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[[Category: Lamont, Y.]]
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[[Category: Papakosta, M]]
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[[Category: Lyons, A J.]]
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[[Category: Rankovic, Z]]
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[[Category: Maclean, J K.F.]]
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[[Category: Smith, L]]
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[[Category: Moir, E M.]]
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[[Category: Morrow, J A.]]
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[[Category: Papakosta, M.]]
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[[Category: Rankovic, Z.]]
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[[Category: Smith, L.]]
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[[Category: Chimera protein]]
[[Category: Chimera protein]]
[[Category: Fusion protein]]
[[Category: Fusion protein]]
[[Category: Membrane protein]]
[[Category: Membrane protein]]
[[Category: Transport protein]]
[[Category: Transport protein]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Sep 29 07:44:32 2010''
 

Current revision

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

3o2a, resolution 1.90Å

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