3b7d

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[[Image:3b7d.gif|left|200px]]
 
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{{Structure
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==Crystal structure of the GLUR2 ligand binding core (HS1S2J) in complex with CNQX at 2.5 A resolution==
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|PDB= 3b7d |SIZE=350|CAPTION= <scene name='initialview01'>3b7d</scene>, resolution 2.50&Aring;
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<StructureSection load='3b7d' size='340' side='right'caption='[[3b7d]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
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|SITE=
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== Structural highlights ==
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|LIGAND= <scene name='pdbligand=CNI:7-NITRO-2,3-DIOXO-2,3-DIHYDROQUINOXALINE-6-CARBONITRILE'>CNI</scene>
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<table><tr><td colspan='2'>[[3b7d]] is a 8 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=3B7D OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3B7D FirstGlance]. <br>
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|ACTIVITY=
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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]] 2.5&#8491;</td></tr>
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|GENE= Gria2, Glur2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus])
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CNI:7-NITRO-2,3-DIOXO-2,3-DIHYDROQUINOXALINE-6-CARBONITRILE'>CNI</scene></td></tr>
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|DOMAIN=
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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=3b7d FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3b7d OCA], [https://pdbe.org/3b7d PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3b7d RCSB], [https://www.ebi.ac.uk/pdbsum/3b7d PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3b7d ProSAT]</span></td></tr>
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|RELATEDENTRY=[[1ftj|1FTJ]], [[1ftm|1FTM]], [[1fto|1FTO]], [[1ftl|1FTL]]
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</table>
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3b7d FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3b7d OCA], [http://www.ebi.ac.uk/pdbsum/3b7d PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=3b7d RCSB]</span>
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== Function ==
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}}
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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/b7/3b7d_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=3b7d 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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Quinoxalinedione compounds such as 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) are the most commonly used alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists. However, we find that in the presence of transmembrane AMPA receptor regulatory proteins (TARPs), which are AMPA receptor auxiliary subunits, CNQX acts as a partial agonist. CNQX induced small depolarizing currents in neurons of the central nervous system, and reconstitution of this agonist activity required coexpression of TARPs. A crystal structure of CNQX bound to the TARP-less AMPA receptor ligand-binding domain showed that, although CNQX induces partial domain closure, this movement is not transduced into linker separation, suggesting that TARPs may increase agonist efficacy by strengthening the coupling between domain closure and channel opening. Our results demonstrate that the presence of an auxiliary subunit can determine whether a compound functions as an agonist or antagonist.
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'''Crystal structure of the GLUR2 ligand binding core (HS1S2J) in complex with CNQX at 2.5 A resolution'''
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TARP auxiliary subunits switch AMPA receptor antagonists into partial agonists.,Menuz K, Stroud RM, Nicoll RA, Hays FA Science. 2007 Nov 2;318(5851):815-7. PMID:17975069<ref>PMID:17975069</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 3b7d" style="background-color:#fffaf0;"></div>
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==Overview==
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==See Also==
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Quinoxalinedione compounds such as 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) are the most commonly used alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists. However, we find that in the presence of transmembrane AMPA receptor regulatory proteins (TARPs), which are AMPA receptor auxiliary subunits, CNQX acts as a partial agonist. CNQX induced small depolarizing currents in neurons of the central nervous system, and reconstitution of this agonist activity required coexpression of TARPs. A crystal structure of CNQX bound to the TARP-less AMPA receptor ligand-binding domain showed that, although CNQX induces partial domain closure, this movement is not transduced into linker separation, suggesting that TARPs may increase agonist efficacy by strengthening the coupling between domain closure and channel opening. Our results demonstrate that the presence of an auxiliary subunit can determine whether a compound functions as an agonist or antagonist.
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*[[Glutamate receptor 3D structures|Glutamate receptor 3D structures]]
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== References ==
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==About this Structure==
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<references/>
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3B7D is a [[Single protein]] structure of 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=3B7D OCA].
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__TOC__
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</StructureSection>
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==Reference==
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[[Category: Large Structures]]
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TARP auxiliary subunits switch AMPA receptor antagonists into partial agonists., Menuz K, Stroud RM, Nicoll RA, Hays FA, Science. 2007 Nov 2;318(5851):815-7. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17975069 17975069]
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[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Single protein]]
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[[Category: Hays FA]]
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[[Category: CSMP, Center for Structures of Membrane Proteins.]]
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[[Category: Hays, F A.]]
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[[Category: alternative splicing]]
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[[Category: cell junction]]
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[[Category: center for structures of membrane protein]]
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[[Category: cnqx]]
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[[Category: csmp]]
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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: lipoprotein]]
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[[Category: palmitate]]
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[[Category: phosphorylation]]
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[[Category: postsynaptic cell membrane]]
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[[Category: protein structure initiative]]
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[[Category: psi-2]]
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[[Category: receptor]]
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[[Category: rna editing]]
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[[Category: s1s2]]
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[[Category: structural genomic]]
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[[Category: synapse]]
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[[Category: transmembrane]]
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[[Category: transport]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:23:46 2008''
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Current revision

Crystal structure of the GLUR2 ligand binding core (HS1S2J) in complex with CNQX at 2.5 A resolution

PDB ID 3b7d

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