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| | <StructureSection load='3r7x' size='340' side='right'caption='[[3r7x]], [[Resolution|resolution]] 2.10Å' scene=''> | | <StructureSection load='3r7x' size='340' side='right'caption='[[3r7x]], [[Resolution|resolution]] 2.10Å' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[3r7x]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3R7X OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3R7X FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[3r7x]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3R7X OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3R7X 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=QSN:N-[6-(1H-IMIDAZOL-1-YL)-7-NITRO-2,4-DIOXO-1,4-DIHYDROQUINAZOLIN-3(2H)-YL]METHANESULFONAMIDE'>QSN</scene></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.1Å</td></tr> |
| - | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2cmo|2cmo]]</td></tr>
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=QSN:N-[6-(1H-IMIDAZOL-1-YL)-7-NITRO-2,4-DIOXO-1,4-DIHYDROQUINAZOLIN-3(2H)-YL]METHANESULFONAMIDE'>QSN</scene></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=3r7x FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3r7x OCA], [http://pdbe.org/3r7x PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3r7x RCSB], [http://www.ebi.ac.uk/pdbsum/3r7x PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3r7x ProSAT]</span></td></tr> | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3r7x FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3r7x OCA], [https://pdbe.org/3r7x PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3r7x RCSB], [https://www.ebi.ac.uk/pdbsum/3r7x PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3r7x ProSAT]</span></td></tr> |
| | </table> | | </table> |
| | == Function == | | == Function == |
| - | [[http://www.uniprot.org/uniprot/GRIA2_HUMAN GRIA2_HUMAN]] 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:20614889</ref> | + | [https://www.uniprot.org/uniprot/GRIA2_HUMAN GRIA2_HUMAN] 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:20614889</ref> |
| | <div style="background-color:#fffaf0;"> | | <div style="background-color:#fffaf0;"> |
| | == Publication Abstract from PubMed == | | == Publication Abstract from PubMed == |
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| | __TOC__ | | __TOC__ |
| | </StructureSection> | | </StructureSection> |
| - | [[Category: Human]] | + | [[Category: Homo sapiens]] |
| | [[Category: Large Structures]] | | [[Category: Large Structures]] |
| - | [[Category: Kallen, J]] | + | [[Category: Kallen J]] |
| - | [[Category: Ion channel]]
| + | |
| - | [[Category: Ionic channel]]
| + | |
| - | [[Category: Postsynaptic membrane]]
| + | |
| - | [[Category: Transmembrane]]
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| - | [[Category: Transport protein]]
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| Structural highlights
Function
GRIA2_HUMAN 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.[1]
Publication Abstract from PubMed
Quinazoline-2,4-diones with a sulfonamide group attached to the N(3) ring atom constitute a novel class of competitive AMPA receptor antagonists. One of the synthesized compounds, 28, shows nanomolar receptor affinity, whereas other examples of the series display oral anticonvulsant activity in animal models.
Quinazolinedione sulfonamides: A novel class of competitive AMPA receptor antagonists with oral activity.,Koller M, Lingenhoehl K, Schmutz M, Vranesic IT, Kallen J, Auberson YP, Carcache DA, Mattes H, Ofner S, Orain D, Urwyler S Bioorg Med Chem Lett. 2011 Apr 8. PMID:21531559[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Ward SE, Harries M, Aldegheri L, Andreotti D, Ballantine S, Bax BD, Harris AJ, Harker AJ, Lund J, Melarange R, Mingardi A, Mookherjee C, Mosley J, Neve M, Oliosi B, Profeta R, Smith KJ, Smith PW, Spada S, Thewlis KM, Yusaf SP. Discovery of N-[(2S)-5-(6-Fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfo namide, a Novel Clinical AMPA Receptor Positive Modulator. J Med Chem. 2010 Jul 8. PMID:20614889 doi:10.1021/jm1005429
- ↑ Koller M, Lingenhoehl K, Schmutz M, Vranesic IT, Kallen J, Auberson YP, Carcache DA, Mattes H, Ofner S, Orain D, Urwyler S. Quinazolinedione sulfonamides: A novel class of competitive AMPA receptor antagonists with oral activity. Bioorg Med Chem Lett. 2011 Apr 8. PMID:21531559 doi:10.1016/j.bmcl.2011.04.017
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