3ua8 - Revision history

OCA at 13:52, 14 March 2024

OCA — Thu, 14 Mar 2024 13:52:31 GMT

←Older revision		Revision as of 13:52, 14 March 2024
Line 3:		Line 3:
	<StructureSection load='3ua8' size='340' side='right'caption='[[3ua8]], [[Resolution\|resolution]] 1.90Å' scene=''>		<StructureSection load='3ua8' size='340' side='right'caption='[[3ua8]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<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>	+	<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>
-	</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>~~	+	</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution\|Resolution]] 1.9Å</td></tr>
-	~~<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>~~	+	<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>
-	~~<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>	+
	<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 ==
-	[[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>	+	[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;">~~	+
-	~~== Publication Abstract from PubMed ==~~	+
-	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.	+
-		+
-	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 MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>~~	+
-	~~</div>~~	+
-	~~<div class="pdbe-citations 3ua8" style="background-color:#fffaf0;"></div~~>	+

	==See Also==		==See Also==
Line 27:		Line 17:
	__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]]~~	+
-	~~[[Category: Transport protein-antagonist complex~~]]	+

OCA at 06:04, 13 July 2022

OCA — Wed, 13 Jul 2022 06:04:42 GMT

←Older revision		Revision as of 06:04, 13 July 2022
Line 1:		Line 1:

	==Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2==		==Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2==
-	<StructureSection load='3ua8' size='340' side='right' caption='[[3ua8]], [[Resolution\|resolution]] 1.90Å' scene=''>	+	<StructureSection load='3ua8' size='340' side='right'caption='[[3ua8]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3ua8]] is a 1 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=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 [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>
-	</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>	+	</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>
-	<tr id='related'><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"><div style='overflow: auto; max-height: 3em;'>[[3r7x\|3r7x]]</div></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 HUMAN])</td></tr>	+	<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>
-	<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~~://pdbe.org/3ua8 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3ua8 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3ua8 PDBsum], [~~http~~://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 ==
-	[[~~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 ==
Line 20:		Line 20:
	</div>		</div>
	<div class="pdbe-citations 3ua8" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 3ua8" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Glutamate receptor 3D structures\|Glutamate receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
Line 25:		Line 28:
	</StructureSection>		</StructureSection>
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Kallen, J]]		[[Category: Kallen, J]]
	[[Category: Ion channel]]		[[Category: Ion channel]]

OCA at 05:25, 16 November 2017

OCA — Thu, 16 Nov 2017 05:25:54 GMT

←Older revision		Revision as of 05:25, 16 November 2017
Line 20:		Line 20:
	</div>		</div>
	<div class="pdbe-citations 3ua8" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 3ua8" style="background-color:#fffaf0;"></div>
-
-	==See Also==
-	*[[Ionotropic Glutamate Receptors\|Ionotropic Glutamate Receptors]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 09:19, 5 August 2016

OCA — Fri, 05 Aug 2016 09:19:34 GMT

←Older revision		Revision as of 09:19, 5 August 2016
Line 1:		Line 1:
		+
	==Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2==		==Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2==
	<StructureSection load='3ua8' size='340' side='right' caption='[[3ua8]], [[Resolution\|resolution]] 1.90Å' scene=''>		<StructureSection load='3ua8' size='340' side='right' caption='[[3ua8]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== 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/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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3UA8 FirstGlance]. <br>
	</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>		</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 id='related'><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 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 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 HUMAN])</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>	+	<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://pdbe.org/3ua8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3ua8 RCSB], [http://www.ebi.ac.uk/pdbsum/3ua8 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3ua8 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 18:		Line 19:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
		+	<div class="pdbe-citations 3ua8" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 25:		Line 27:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Kallen, J]]		[[Category: Kallen, J]]
	[[Category: Ion channel]]		[[Category: Ion channel]]

OCA at 01:07, 25 December 2014

OCA — Thu, 25 Dec 2014 01:07:27 GMT

←Older revision		Revision as of 01:07, 25 December 2014
Line 3:		Line 3:
	== 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><br>	+	</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 ==
Line 14:		Line 16:
	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 ~~MEDLINEÂ®~~/~~PubMedÂ®~~, a database of the U.S. National Library of Medicine.<br>	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>

Line 24:		Line 26:
	</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]]

OCA at 05:44, 5 June 2014

OCA — Thu, 05 Jun 2014 05:44:33 GMT

←Older revision		Revision as of 05:44, 5 June 2014
Line 1:		Line 1:
-	[[~~Image:~~3ua8.~~png~~\|~~left~~\|~~200px~~]]	+	==Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2==
		+	<StructureSection load='3ua8' size='340' side='right' caption='[[3ua8]], [[Resolution\|resolution]] 1.90Å' scene=''>
		+	== 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>
		+	</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><br>
		+	<tr><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><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>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	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.

-	<!--	+	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>
-	~~The line below this paragraph~~, ~~containing "STRUCTURE_3ua8"~~, ~~creates the "Structure Box" on the page.~~	+
-	~~You may change the PDB parameter (which sets the PDB file loaded into the applet)~~	+
-	~~or the SCENE parameter (which sets the initial scene displayed when the page is loaded)~~,	+
-	~~or leave the SCENE parameter empty for the default display~~.	+
-	-->	+
-	~~{{STRUCTURE_3ua8\| PDB=3ua8 \| SCENE= }}~~	+

-	~~===Crystal Structure Analysis of~~ a ~~6-Amino Quinazolinedione Sulfonamide bound to human GluR2===~~	+	From MEDLINEÂ®/PubMedÂ®, a database of the U.S. National Library of Medicine.<br>
		+	</div>

-		+	==See Also==
-	~~<!--~~	+	*[[Ionotropic Glutamate Receptors\|Ionotropic Glutamate Receptors]]
-	~~The line below this paragraph, {{ABSTRACT_PUBMED_22197388}}, adds the Publication Abstract to the page~~	+	== References ==
-	~~(as it appears on PubMed at http://www.pubmed.gov), where 22197388 is the PubMed ID number.~~	+	<references/>
-	~~-->~~	+	__TOC__
-	~~{{ABSTRACT_PUBMED_22197388}}~~	+	</StructureSection>
-		+
-	==~~About this Structure~~==	+
-	[[~~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].	+
-		+
-	==~~Reference~~==	+
-	<~~ref group="xtra">PMID:022197388<~~/~~ref~~><~~references group="xtra"~~/>	+
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Kallen, J.]]		[[Category: Kallen, J.]]

OCA at 06:18, 11 January 2012

OCA — Wed, 11 Jan 2012 06:18:19 GMT

←Older revision		Revision as of 06:18, 11 January 2012
Line 1:		Line 1:
-	~~'''Unreleased structure'''~~	+	[[Image:3ua8.png\|left\|200px]]

-	The ~~entry 3ua8~~ is ~~ON HOLD~~ ~~until Paper Publication~~	+	<!--
		+	The line below this paragraph, containing "STRUCTURE_3ua8", creates the "Structure Box" on the page.
		+	You may change the PDB parameter (which sets the PDB file loaded into the applet)
		+	or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
		+	or leave the SCENE parameter empty for the default display.
		+	-->
		+	{{STRUCTURE_3ua8\| PDB=3ua8 \| SCENE= }}

-	~~Authors: Kallen, J.~~	+	===Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2===

-	~~Description~~: ~~Crystal~~ Structure ~~Analysis of~~ a 6-~~Amino Quinazolinedione Sulfonamide bound to human GluR2~~	+
		+	<!--
		+	The line below this paragraph, {{ABSTRACT_PUBMED_22197388}}, adds the Publication Abstract to the page
		+	(as it appears on PubMed at http://www.pubmed.gov), where 22197388 is the PubMed ID number.
		+	-->
		+	{{ABSTRACT_PUBMED_22197388}}
		+
		+	==About this Structure==
		+	[[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].
		+
		+	==Reference==
		+	<ref group="xtra">PMID:022197388</ref><references group="xtra"/>
		+	[[Category: Homo sapiens]]
		+	[[Category: Kallen, J.]]
		+	[[Category: Ion channel]]
		+	[[Category: Ionic channel]]
		+	[[Category: Postsynaptic membrane]]
		+	[[Category: Transmembrane]]
		+	[[Category: Transport protein-antagonist complex]]

OCA at 11:15, 9 November 2011

OCA — Wed, 09 Nov 2011 11:15:26 GMT

←Older revision		Revision as of 11:15, 9 November 2011
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 3ua8 is ON HOLD	+	The entry 3ua8 is ON HOLD until Paper Publication

	Authors: Kallen, J.		Authors: Kallen, J.

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

OCA: Protected "3ua8" [edit=sysop:move=sysop]

OCA — Sun, 30 Oct 2011 08:56:48 GMT

Protected "3ua8" [edit=sysop:move=sysop]

←Older revision

Revision as of 08:56, 30 October 2011

OCA: New page: '''Unreleased structure''' The entry 3ua8 is ON HOLD Authors: Kallen, J. Description: Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2

OCA — Sun, 30 Oct 2011 08:56:47 GMT

New page: '''Unreleased structure''' The entry 3ua8 is ON HOLD Authors: Kallen, J. Description: Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2

New page

'''Unreleased structure'''

The entry 3ua8 is ON HOLD

Authors: Kallen, J.

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