3ua8

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<StructureSection load='3ua8' size='340' side='right'caption='[[3ua8]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
<StructureSection load='3ua8' size='340' side='right'caption='[[3ua8]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[3ua8]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3UA8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3UA8 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[3ua8]] is a 1 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=3UA8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3UA8 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=08W:N-METHYL-1-{3-[(METHYLSULFONYL)AMINO]-2,4-DIOXO-7-(TRIFLUOROMETHYL)-1,2,3,4-TETRAHYDROQUINAZOLIN-6-YL}-1H-IMIDAZOLE-4-CARBOXAMIDE'>08W</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]] 1.9&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[3r7x|3r7x]]</div></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=08W:N-METHYL-1-{3-[(METHYLSULFONYL)AMINO]-2,4-DIOXO-7-(TRIFLUOROMETHYL)-1,2,3,4-TETRAHYDROQUINAZOLIN-6-YL}-1H-IMIDAZOLE-4-CARBOXAMIDE'>08W</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">GRIA2, GLUR2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=3ua8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ua8 OCA], [https://pdbe.org/3ua8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3ua8 RCSB], [https://www.ebi.ac.uk/pdbsum/3ua8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3ua8 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=3ua8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ua8 OCA], [https://pdbe.org/3ua8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3ua8 RCSB], [https://www.ebi.ac.uk/pdbsum/3ua8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3ua8 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[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>
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[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>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By modulating physico-chemical properties, compound 29 was identified with a low ED(50) of 5.5mg/kg in an animal model of anticonvulsant activity after oral dosage.
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6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.,Orain D, Ofner S, Koller M, Carcache DA, Froestl W, Allgeier H, Rasetti V, Nozulak J, Mattes H, Soldermann N, Floersheim P, Desrayaud S, Kallen J, Lingenhoehl K, Urwyler S Bioorg Med Chem Lett. 2011 Dec 8. PMID:22197388<ref>PMID:22197388</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 3ua8" style="background-color:#fffaf0;"></div>
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==See Also==
==See Also==
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Kallen, J]]
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[[Category: Kallen J]]
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[[Category: Ion channel]]
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[[Category: Ionic channel]]
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[[Category: Postsynaptic membrane]]
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[[Category: Transmembrane]]
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[[Category: Transport protein-antagonist complex]]
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Revision as of 13:52, 14 March 2024

Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2

PDB ID 3ua8

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