3bfu

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[[Image:3bfu.png|left|200px]]
 
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{{STRUCTURE_3bfu| PDB=3bfu | SCENE= }}
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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 [https://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 [https://proteopedia.org/fgij/fg.htm?mol=3BFU 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]] 1.95&#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=R2P:(2R)-2-AMINO-3-(4-HYDROXY-1,2,5-THIADIAZOL-3-YL)PROPANOIC+ACID'>R2P</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=3bfu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3bfu OCA], [https://pdbe.org/3bfu PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3bfu RCSB], [https://www.ebi.ac.uk/pdbsum/3bfu PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3bfu 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/bf/3bfu_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=3bfu 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 of the ligand-binding core of GluR2 in complex with the agonist (R)-TDPA at 1.95 A resolution===
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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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{{ABSTRACT_PUBMED_18269227}}
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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 3bfu" style="background-color:#fffaf0;"></div>
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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==
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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:018269227</ref><ref group="xtra">PMID:011086992</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: Beich-Frandsen, M.]]
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[[Category: Beich-Frandsen M]]
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[[Category: Gajhede, M.]]
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[[Category: Gajhede M]]
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[[Category: Kastrup, J S.]]
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[[Category: Kastrup JS]]
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[[Category: Mirza, O.]]
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[[Category: Mirza O]]
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[[Category: Vestergaard, B.]]
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[[Category: Vestergaard B]]
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[[Category: Agonist]]
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[[Category: Ampa receptor]]
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[[Category: Cell junction]]
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[[Category: Endoplasmic reticulum]]
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[[Category: Glur2]]
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[[Category: Glycoprotein]]
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[[Category: Ion transport]]
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[[Category: Ionic channel]]
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[[Category: Ligand-binding core]]
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[[Category: Lipoprotein]]
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[[Category: Membrane]]
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[[Category: Membrane protein]]
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[[Category: Palmitate]]
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[[Category: Phosphoprotein]]
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[[Category: Postsynaptic cell membrane]]
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[[Category: Rna editing]]
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[[Category: Synapse]]
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[[Category: Transmembrane]]
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[[Category: Transport]]
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Current revision

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

PDB ID 3bfu

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