3o2a
From Proteopedia
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| - | [[ | + | ==Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator== |
| + | <StructureSection load='3o2a' size='340' side='right' caption='[[3o2a]], [[Resolution|resolution]] 1.90Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[3o2a]] 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=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> | ||
| + | </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> | ||
| + | <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> | ||
| + | <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> | ||
| + | <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://www.rcsb.org/pdb/explore.do?structureId=3o2a RCSB], [http://www.ebi.ac.uk/pdbsum/3o2a PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | == Evolutionary Conservation == | ||
| + | [[Image:Consurf_key_small.gif|200px|right]] | ||
| + | Check<jmol> | ||
| + | <jmolCheckbox> | ||
| + | <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/o2/3o2a_consurf.spt"</scriptWhenChecked> | ||
| + | <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked> | ||
| + | <text>to colour the structure by Evolutionary Conservation</text> | ||
| + | </jmolCheckbox> | ||
| + | </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/chain_selection.php?pdb_ID=2ata ConSurf]. | ||
| + | <div style="clear:both"></div> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | 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. | ||
| - | + | 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> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
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==See Also== | ==See Also== | ||
*[[Ionotropic Glutamate Receptors|Ionotropic Glutamate Receptors]] | *[[Ionotropic Glutamate Receptors|Ionotropic Glutamate Receptors]] | ||
| - | + | == References == | |
| - | == | + | <references/> |
| - | < | + | __TOC__ |
| + | </StructureSection> | ||
[[Category: Rattus norvegicus]] | [[Category: Rattus norvegicus]] | ||
| - | [[Category: Basten, S | + | [[Category: Basten, S]] |
| - | [[Category: Campbell, R A | + | [[Category: Campbell, R A]] |
| - | [[Category: Cumming, I A | + | [[Category: Cumming, I A]] |
| - | [[Category: Gillen, K J | + | [[Category: Gillen, K J]] |
| - | [[Category: Gillespie, J | + | [[Category: Gillespie, J]] |
| - | [[Category: Jamieson, C | + | [[Category: Jamieson, C]] |
| - | [[Category: Kazemier, B | + | [[Category: Kazemier, B]] |
| - | [[Category: Kiczun, M | + | [[Category: Kiczun, M]] |
| - | [[Category: Lamont, Y | + | [[Category: Lamont, Y]] |
| - | [[Category: Lyons, A J | + | [[Category: Lyons, A J]] |
| - | [[Category: Maclean, J K.F | + | [[Category: Maclean, J K.F]] |
| - | [[Category: Moir, E M | + | [[Category: Moir, E M]] |
| - | [[Category: Morrow, J A | + | [[Category: Morrow, J A]] |
| - | [[Category: Papakosta, M | + | [[Category: Papakosta, M]] |
| - | [[Category: Rankovic, Z | + | [[Category: Rankovic, Z]] |
| - | [[Category: Smith, L | + | [[Category: Smith, L]] |
[[Category: Chimera protein]] | [[Category: Chimera protein]] | ||
[[Category: Fusion protein]] | [[Category: Fusion protein]] | ||
[[Category: Membrane protein]] | [[Category: Membrane protein]] | ||
[[Category: Transport protein]] | [[Category: Transport protein]] | ||
Revision as of 10:58, 9 December 2014
Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator
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Categories: Rattus norvegicus | Basten, S | Campbell, R A | Cumming, I A | Gillen, K J | Gillespie, J | Jamieson, C | Kazemier, B | Kiczun, M | Lamont, Y | Lyons, A J | Maclean, J K.F | Moir, E M | Morrow, J A | Papakosta, M | Rankovic, Z | Smith, L | Chimera protein | Fusion protein | Membrane protein | Transport protein
