2xxh

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==CRYSTAL STRUCTURE OF 1-(4-(2-OXO-2-(1-PYRROLIDINYL)ETHYL)PHENYL)-3-(TRIFLUOROMETHYL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE IN COMPLEX WITH THE LIGAND BINDING DOMAIN OF THE RAT GLUA2 RECEPTOR AND GLUTAMATE AT 1.5A RESOLUTION.==
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==Crystal structure of 1-(4-(2-oxo-2-(1-pyrrolidinyl)ethyl)phenyl)-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazole in complex with the ligand binding domain of the Rat GluA2 receptor and glutamate at 1.5A resolution.==
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<StructureSection load='2xxh' size='340' side='right' caption='[[2xxh]], [[Resolution|resolution]] 1.50&Aring;' scene=''>
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<StructureSection load='2xxh' size='340' side='right'caption='[[2xxh]], [[Resolution|resolution]] 1.50&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[2xxh]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Buffalo_rat Buffalo rat]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2XXH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2XXH FirstGlance]. <br>
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<table><tr><td colspan='2'>[[2xxh]] is a 3 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=2XXH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2XXH FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1NG:1-{4-[2-OXO-2-(1-PYRROLIDINYL)ETHYL]PHENYL}-3-(+TRIFLUOROMETHYL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE'>1NG</scene>, <scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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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]] 1.5&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1m5c|1m5c]], [[1p1o|1p1o]], [[1mqh|1mqh]], [[1lb8|1lb8]], [[1p1u|1p1u]], [[1mm7|1mm7]], [[1nnp|1nnp]], [[1m5d|1m5d]], [[1syi|1syi]], [[1p1q|1p1q]], [[1mqd|1mqd]], [[1p1w|1p1w]], [[1mxu|1mxu]], [[1my4|1my4]], [[2i3v|2i3v]], [[2i3w|2i3w]], [[1n0t|1n0t]], [[2xxi|2xxi]], [[1mqi|1mqi]], [[1ftk|1ftk]], [[1my3|1my3]], [[2anj|2anj]], [[1fto|1fto]], [[1mxv|1mxv]], [[1p1n|1p1n]], [[2xx9|2xx9]], [[1ftj|1ftj]], [[1syh|1syh]], [[1m5e|1m5e]], [[1lbb|1lbb]], [[1fw0|1fw0]], [[1mxz|1mxz]], [[1mxy|1mxy]], [[1mqg|1mqg]], [[2xx8|2xx8]], [[2aix|2aix]], [[1m5b|1m5b]], [[1mxw|1mxw]], [[1ms7|1ms7]], [[2xx7|2xx7]], [[1my0|1my0]], [[1m5f|1m5f]], [[1xhy|1xhy]], [[1my1|1my1]], [[1mm6|1mm6]], [[2cmo|2cmo]], [[2al4|2al4]], [[1wvj|1wvj]], [[2uxa|2uxa]], [[1ftl|1ftl]], [[1mxx|1mxx]], [[1ftm|1ftm]], [[1lb9|1lb9]], [[1lbc|1lbc]], [[1nnk|1nnk]], [[1my2|1my2]], [[1mqj|1mqj]], [[2al5|2al5]], [[1gr2|1gr2]]</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=1NG:1-{4-[2-OXO-2-(1-PYRROLIDINYL)ETHYL]PHENYL}-3-(+TRIFLUOROMETHYL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE'>1NG</scene>, <scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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<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=2xxh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xxh OCA], [http://pdbe.org/2xxh PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2xxh RCSB], [http://www.ebi.ac.uk/pdbsum/2xxh PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2xxh ProSAT]</span></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=2xxh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xxh OCA], [https://pdbe.org/2xxh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2xxh RCSB], [https://www.ebi.ac.uk/pdbsum/2xxh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2xxh ProSAT]</span></td></tr>
</table>
</table>
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== Function ==
 
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[[http://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>
 
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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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]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Buffalo rat]]
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[[Category: Large Structures]]
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[[Category: Aldegheri, L]]
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[[Category: Rattus norvegicus]]
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[[Category: Austin, N E]]
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[[Category: Aldegheri L]]
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[[Category: Ballantine, S]]
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[[Category: Austin NE]]
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[[Category: Ballini, E]]
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[[Category: Ballantine S]]
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[[Category: Bax, B D]]
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[[Category: Ballini E]]
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[[Category: Bradley, D M]]
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[[Category: Bax BD]]
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[[Category: Clarke, B P]]
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[[Category: Bradley DM]]
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[[Category: Dalnegro, G]]
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[[Category: Clarke BP]]
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[[Category: Harries, M]]
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[[Category: DalNegro G]]
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[[Category: Harris, A J]]
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[[Category: Harries M]]
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[[Category: Harrison, S A]]
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[[Category: Harris AJ]]
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[[Category: Melarange, R A]]
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[[Category: Harrison SA]]
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[[Category: Mookherjee, C]]
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[[Category: Melarange RA]]
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[[Category: Mosley, J]]
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[[Category: Mookherjee C]]
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[[Category: Oliosi, B]]
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[[Category: Mosley J]]
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[[Category: Smith, K J]]
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[[Category: Oliosi B]]
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[[Category: Thewlis, K M]]
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[[Category: Smith KJ]]
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[[Category: Ward, S E]]
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[[Category: Thewlis KM]]
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[[Category: Woollard, P M]]
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[[Category: Ward SE]]
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[[Category: Yusaf, S P]]
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[[Category: Woollard PM]]
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[[Category: Ampa receptor ligand-binding core]]
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[[Category: Yusaf SP]]
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[[Category: Ion channel]]
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[[Category: Transport protein]]
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Current revision

Crystal structure of 1-(4-(2-oxo-2-(1-pyrrolidinyl)ethyl)phenyl)-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazole in complex with the ligand binding domain of the Rat GluA2 receptor and glutamate at 1.5A resolution.

PDB ID 2xxh

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