3o6i
From Proteopedia
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| - | [[ | + | ==Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator== |
| + | <StructureSection load='3o6i' size='340' side='right' caption='[[3o6i]], [[Resolution|resolution]] 1.80Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[3o6i]] 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=3O6I OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3O6I 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=O26:2-[({3-TERT-BUTYL-4-[(METHYLAMINO)METHYL]-1H-PYRAZOL-1-YL}ACETYL)AMINO]-4,5,6,7-TETRAHYDRO-1-BENZOTHIOPHENE-3-CARBOXAMIDE'>O26</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]], [[3o2a|3o2a]], [[3o6g|3o6g]], [[3o6h|3o6h]], [[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=3o6i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3o6i OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3o6i RCSB], [http://www.ebi.ac.uk/pdbsum/3o6i 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/o6/3o6i_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 lead compound 1, we demonstrate how X-ray structural data can be used to understand SAR and expediently optimize bioavailability in a novel series of AMPA receptor modulators, furnishing 5 with improved bioavailability and robust in vivo activity. | ||
| - | + | A novel series of positive modulators of the AMPA receptor: Structure-based lead optimization.,Jamieson C, Campbell RA, Cumming IA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Maclean JK, Martin F, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L Bioorg Med Chem Lett. 2010 Aug 15. PMID:20817521<ref>PMID:20817521</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: 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: Martin, F | + | [[Category: Martin, F]] |
| - | [[Category: Moir, E M | + | [[Category: Moir, E M]] |
| - | [[Category: Morrow, J A | + | [[Category: Morrow, J A]] |
| - | [[Category: Pantling, J | + | [[Category: Pantling, J]] |
| - | [[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 12:08, 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 | 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 | Martin, F | Moir, E M | Morrow, J A | Pantling, J | Rankovic, Z | Smith, L | Chimera protein | Fusion protein | Membrane protein | Transport protein
