3ua8
From Proteopedia
(Difference between revisions)
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[3ua8]] is a 1 chain structure with sequence from [http://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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3UA8 FirstGlance]. <br> | <table><tr><td colspan='2'>[[3ua8]] is a 1 chain structure with sequence from [http://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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3UA8 FirstGlance]. <br> | ||
| - | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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> |
| - | <tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3r7x|3r7x]]</td></tr> | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3r7x|3r7x]]</td></tr> |
| - | <tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">GRIA2, GLUR2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr> | + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">GRIA2, GLUR2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr> |
| - | <tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ua8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ua8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3ua8 RCSB], [http://www.ebi.ac.uk/pdbsum/3ua8 PDBsum]</span></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=3ua8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ua8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3ua8 RCSB], [http://www.ebi.ac.uk/pdbsum/3ua8 PDBsum]</span></td></tr> |
| - | <table> | + | </table> |
| + | == 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> | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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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> | 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> | ||
| - | From | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> |
</div> | </div> | ||
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</StructureSection> | </StructureSection> | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| - | [[Category: Kallen, J | + | [[Category: Kallen, J]] |
[[Category: Ion channel]] | [[Category: Ion channel]] | ||
[[Category: Ionic channel]] | [[Category: Ionic channel]] | ||
Revision as of 01:07, 25 December 2014
Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2
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