3bfu

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[[Image:3bfu.png|left|200px]]
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==Structure of the ligand-binding core of GluR2 in complex with the agonist (R)-TDPA at 1.95 A resolution==
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<StructureSection load='3bfu' size='340' side='right' caption='[[3bfu]], [[Resolution|resolution]] 1.95&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3bfu]] 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=3BFU OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3BFU FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=R2P:(2R)-2-AMINO-3-(4-HYDROXY-1,2,5-THIADIAZOL-3-YL)PROPANOIC+ACID'>R2P</scene><br>
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<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1ftm|1ftm]], [[3bft|3bft]]</td></tr>
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<tr><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>
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3bfu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3bfu OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3bfu RCSB], [http://www.ebi.ac.uk/pdbsum/3bfu PDBsum]</span></td></tr>
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<table>
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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/bf/3bfu_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/chain_selection.php?pdb_ID=2ata 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-type ionotropic glutamate receptors generally display high stereoselectivity in agonist binding. However, the stereoisomers of 2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid (TDPA) have similar enantiopharmacology. To understand this observation, we have determined the X-ray structures of ( R)-TDPA and ( S)-TDPA in complex with the ligand-binding core of iGluR2 and investigated the binding pharmacology at AMPA and kainate receptors. Both enantiomers induce full domain closure in iGluR2 but adopt different conformations when binding to the receptor, which may explain the similar enantiopharmacology.
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{{STRUCTURE_3bfu| PDB=3bfu | SCENE= }}
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Structures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency.,Beich-Frandsen M, Pickering DS, Mirza O, Johansen TN, Greenwood J, Vestergaard B, Schousboe A, Gajhede M, Liljefors T, Kastrup JS J Med Chem. 2008 Mar 13;51(5):1459-63. Epub 2008 Feb 13. PMID:18269227<ref>PMID:18269227</ref>
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===Structure of the ligand-binding core of GluR2 in complex with the agonist (R)-TDPA at 1.95 A resolution===
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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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{{ABSTRACT_PUBMED_18269227}}
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==About this Structure==
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[[3bfu]] 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=3BFU OCA].
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==See Also==
==See Also==
*[[Ionotropic Glutamate Receptors|Ionotropic Glutamate Receptors]]
*[[Ionotropic Glutamate Receptors|Ionotropic Glutamate Receptors]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:018269227</ref><ref group="xtra">PMID:011086992</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
[[Category: Beich-Frandsen, M.]]
[[Category: Beich-Frandsen, M.]]

Revision as of 07:17, 29 September 2014

Structure of the ligand-binding core of GluR2 in complex with the agonist (R)-TDPA at 1.95 A resolution

3bfu, resolution 1.95Å

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