3rtf - Revision history

OCA at 06:44, 27 November 2024

2024-11-27T06:44:43Z

← Older revision		Revision as of 06:44, 27 November 2024
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	== Function ==		== Function ==
	[https://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>		[https://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;">
			== Publication Abstract from PubMed ==
			AMPA receptors are the major excitatory neurotransmitter receptors in the CNS and are involved in numerous neurological disorders. An agonist-binding site is present in each of four subunits that form a functional channel. Binding consists of three steps: docking of agonist to the bi-lobed ligand binding domain (LBD), closure of the LBD, and increased stability of the closed-lobe conformation through interlobe hydrogen bonding. We describe GluA3 single channel currents activated by nitrowillardiine (NO(2)W) and chlorowillardiine (ClW) in the presence of cyclothiazide, in conjunction with crystal structures of GluA2 and GluA3 LBDs bound to fluorowillardiine (FW), ClW, and NO(2)W. When bound to NO(2)W or ClW, the GluA3 channel opens to three conductance levels with comparable open probabilities and displays modal behavior similar to that obtained with glutamate and FW as agonists (Poon et al., 2010). At lower concentrations, ClW evoked an alternate kinetic behavior, consisting of high open probability in lower conductance states. The structure of ClW bound to GluA3 LBD exhibits a unique partially open hydrogen bonding structure that may be associated with these alternative kinetics. NO(2)W evoked longer open times than seen for other agonists in high and very high modes. The structure of GluA2 LBD bound to NO2W exhibits fully closed lobes with additional interlobe interactions mediated by the nitro group. Beyond differences in efficacy between full and partial agonists, the complexities of the single channel behavior of AMPA receptors may also be associated with small interactions that modify the stability of various degrees of closure.

			Mechanisms of Modal Activation of GluA3 Receptors.,Poon K, Ahmed AH, Nowak LM, Oswald RE Mol Pharmacol. 2011 Apr 4. PMID:21464198<ref>PMID:21464198</ref>

			From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
			</div>
			<div class="pdbe-citations 3rtf" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==

OCA at 12:36, 14 March 2024

2024-03-14T12:36:42Z

← Older revision		Revision as of 12:36, 14 March 2024
Line 3:		Line 3:
	<StructureSection load='3rtf' size='340' side='right'caption='[[3rtf]], [[Resolution\|resolution]] 1.70Å' scene=''>		<StructureSection load='3rtf' size='340' side='right'caption='[[3rtf]], [[Resolution\|resolution]] 1.70Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3rtf]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/~~Buffalo_rat Buffalo rat~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RTF OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3RTF FirstGlance]. <br>		<table><tr><td colspan='2'>[[3rtf]] 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=3RTF OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3RTF FirstGlance]. <br>
	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat" id="~~ligandDat~~">~~<scene name='pdbligand=CWD:3~~-~~(5-CHLORO-2~~,~~4-DIOXO-3,4-DIHYDROPYRIMIDIN-~~1~~(2H)-YL)-L-ALANINE'>CWD</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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]] 1.7Å</td></tr>
	<tr id='~~related~~'><td class="sblockLbl"><b>[[~~Related_structure~~\|~~Related~~:]]</b></td><td class="sblockDat"><~~div style~~='~~overflow~~: ~~auto; max~~-~~height: 3em;'>[[3rt6\|3rt6]]~~, ~~[[3rt8\|3rt8]]~~, ~~[[3rtw\|3rtw]]</div~~></td><~~/tr>~~		<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CWD:3-(5-CHLORO-2,4-DIOXO-3,4-DIHYDROPYRIMIDIN-1(2H)-YL)-L-ALANINE'>CWD</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
	~~<tr id~~='~~gene'><td class~~=~~"sblockLbl"><b>[[Gene\|Gene~~:~~]]</b~~></td>~~<td class="sblockDat">GluA2, Glur2, Gria2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat])~~</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=3rtf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rtf OCA], [https://pdbe.org/3rtf PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rtf RCSB], [https://www.ebi.ac.uk/pdbsum/3rtf PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rtf 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=3rtf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rtf OCA], [https://pdbe.org/3rtf PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rtf RCSB], [https://www.ebi.ac.uk/pdbsum/3rtf PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rtf ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[https://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>		[https://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;">~~
	~~== Publication Abstract from PubMed ==~~
	AMPA receptors are the major excitatory neurotransmitter receptors in the CNS and are involved in numerous neurological disorders. An agonist-binding site is present in each of four subunits that form a functional channel. Binding consists of three steps: docking of agonist to the bi-lobed ligand binding domain (LBD), closure of the LBD, and increased stability of the closed-lobe conformation through interlobe hydrogen bonding. We describe GluA3 single channel currents activated by nitrowillardiine (NO(2)W) and chlorowillardiine (ClW) in the presence of cyclothiazide, in conjunction with crystal structures of GluA2 and GluA3 LBDs bound to fluorowillardiine (FW), ClW, and NO(2)W. When bound to NO(2)W or ClW, the GluA3 channel opens to three conductance levels with comparable open probabilities and displays modal behavior similar to that obtained with glutamate and FW as agonists (Poon et al., 2010). At lower concentrations, ClW evoked an alternate kinetic behavior, consisting of high open probability in lower conductance states. The structure of ClW bound to GluA3 LBD exhibits a unique partially open hydrogen bonding structure that may be associated with these alternative kinetics. NO(2)W evoked longer open times than seen for other agonists in high and very high modes. The structure of GluA2 LBD bound to NO2W exhibits fully closed lobes with additional interlobe interactions mediated by the nitro group. Beyond differences in efficacy between full and partial agonists, the complexities of the single channel behavior of AMPA receptors may also be associated with small interactions that modify the stability of various degrees of closure.

	~~Mechanisms of Modal Activation of GluA3 Receptors.,Poon K, Ahmed AH, Nowak LM, Oswald RE Mol Pharmacol. 2011 Apr 4. PMID:21464198<ref>PMID:21464198</ref>~~

	~~From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>~~
	~~</div>~~
	~~<div class="pdbe-citations 3rtf" style="background-color:#fffaf0;"></div~~>

	==See Also==		==See Also==
Line 27:		Line 17:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	~~[[Category: Buffalo rat]]~~
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: ~~Ahmed, A H~~]]		[[Category: Rattus norvegicus]]
	[[Category: ~~Oswald, R E~~]]		[[Category: Ahmed AH]]
	[[Category: ~~Ampa receptor]]~~		[[Category: Oswald RE]]
	~~[[Category: Glur2]]~~
	~~[[Category: Glutamate receptor]]~~
	~~[[Category: Neurotransmitter receptor]]~~
	~~[[Category: S1s2]]~~
	~~[[Category: Transport protein~~]]

OCA at 10:24, 22 June 2022

2022-06-22T10:24:29Z

← Older revision		Revision as of 10:24, 22 June 2022
Line 1:		Line 1:

	==Chlorowillardiine bound to the ligand binding domain of GluA2==		==Chlorowillardiine bound to the ligand binding domain of GluA2==
	<StructureSection load='3rtf' size='340' side='right' caption='[[3rtf]], [[Resolution\|resolution]] 1.70Å' scene=''>		<StructureSection load='3rtf' size='340' side='right'caption='[[3rtf]], [[Resolution\|resolution]] 1.70Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3rtf]] 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=3RTF OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3RTF FirstGlance]. <br>		<table><tr><td colspan='2'>[[3rtf]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Buffalo_rat Buffalo rat]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RTF OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3RTF FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CWD:3-(5-CHLORO-2,4-DIOXO-3,4-DIHYDROPYRIMIDIN-1(2H)-YL)-L-ALANINE'>CWD</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CWD:3-(5-CHLORO-2,4-DIOXO-3,4-DIHYDROPYRIMIDIN-1(2H)-YL)-L-ALANINE'>CWD</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3rt6\|3rt6]], [[3rt8\|3rt8]], [[3rtw\|3rtw]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[3rt6\|3rt6]], [[3rt8\|3rt8]], [[3rtw\|3rtw]]</div></td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">GluA2, Glur2, Gria2 ([~~http~~://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">GluA2, Glur2, Gria2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat])</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=3rtf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rtf OCA], [~~http~~://pdbe.org/3rtf PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3rtf RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3rtf PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=3rtf 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=3rtf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rtf OCA], [https://pdbe.org/3rtf PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rtf RCSB], [https://www.ebi.ac.uk/pdbsum/3rtf PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rtf ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[~~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>		[[https://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 ==
Line 20:		Line 20:
	</div>		</div>
	<div class="pdbe-citations 3rtf" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 3rtf" 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: Buffalo rat]]		[[Category: Buffalo rat]]
			[[Category: Large Structures]]
	[[Category: Ahmed, A H]]		[[Category: Ahmed, A H]]
	[[Category: Oswald, R E]]		[[Category: Oswald, R E]]

OCA at 05:22, 16 November 2017

2017-11-16T05:22:38Z

← Older revision		Revision as of 05:22, 16 November 2017
Line 20:		Line 20:
	</div>		</div>
	<div class="pdbe-citations 3rtf" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 3rtf" style="background-color:#fffaf0;"></div>

	~~==See Also==~~
	*[[Ionotropic Glutamate Receptors\|Ionotropic Glutamate Receptors]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 14:27, 5 August 2016

2016-08-05T14:27:04Z

← Older revision		Revision as of 14:27, 5 August 2016
Line 1:		Line 1:

	==Chlorowillardiine bound to the ligand binding domain of GluA2==		==Chlorowillardiine bound to the ligand binding domain of GluA2==
	<StructureSection load='3rtf' size='340' side='right' caption='[[3rtf]], [[Resolution\|resolution]] 1.70Å' scene=''>		<StructureSection load='3rtf' size='340' side='right' caption='[[3rtf]], [[Resolution\|resolution]] 1.70Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3rtf]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/~~Rattus_norvegicus Rattus norvegicus~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RTF OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3RTF FirstGlance]. <br>		<table><tr><td colspan='2'>[[3rtf]] 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=3RTF OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3RTF FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CWD:3-(5-CHLORO-2,4-DIOXO-3,4-DIHYDROPYRIMIDIN-1(2H)-YL)-L-ALANINE'>CWD</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CWD:3-(5-CHLORO-2,4-DIOXO-3,4-DIHYDROPYRIMIDIN-1(2H)-YL)-L-ALANINE'>CWD</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3rt6\|3rt6]], [[3rt8\|3rt8]], [[3rtw\|3rtw]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3rt6\|3rt6]], [[3rt8\|3rt8]], [[3rtw\|3rtw]]</td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">GluA2, Glur2, Gria2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 ~~Rattus norvegicus~~])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">GluA2, Glur2, Gria2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat])</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=3rtf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rtf OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rtf RCSB], [http://www.ebi.ac.uk/pdbsum/3rtf 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=3rtf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rtf OCA], [http://pdbe.org/3rtf PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3rtf RCSB], [http://www.ebi.ac.uk/pdbsum/3rtf PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3rtf ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
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	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 3rtf" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Rattus norvegicus~~]]		[[Category: Buffalo rat]]
	[[Category: Ahmed, A H]]		[[Category: Ahmed, A H]]
	[[Category: Oswald, R E]]		[[Category: Oswald, R E]]

OCA at 19:33, 25 December 2014

2014-12-25T19:33:58Z

← Older revision		Revision as of 19:33, 25 December 2014
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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=3rtf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rtf OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rtf RCSB], [http://www.ebi.ac.uk/pdbsum/3rtf 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=3rtf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rtf OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rtf RCSB], [http://www.ebi.ac.uk/pdbsum/3rtf PDBsum]</span></td></tr>
	</table>		</table>
			== Function ==
			[[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 ==

OCA at 12:33, 9 December 2014

2014-12-09T12:33:08Z

← Older revision		Revision as of 12:33, 9 December 2014
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	[[~~Image~~:~~3rtf~~.~~png~~\|~~left~~\|~~200px~~]]		==Chlorowillardiine bound to the ligand binding domain of GluA2==
			<StructureSection load='3rtf' size='340' side='right' caption='[[3rtf]], [[Resolution\|resolution]] 1.70Å' scene=''>
			== Structural highlights ==
			<table><tr><td colspan='2'>[[3rtf]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RTF OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3RTF FirstGlance]. <br>
			</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CWD:3-(5-CHLORO-2,4-DIOXO-3,4-DIHYDROPYRIMIDIN-1(2H)-YL)-L-ALANINE'>CWD</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
			<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3rt6\|3rt6]], [[3rt8\|3rt8]], [[3rtw\|3rtw]]</td></tr>
			<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">GluA2, Glur2, Gria2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus])</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=3rtf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rtf OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rtf RCSB], [http://www.ebi.ac.uk/pdbsum/3rtf PDBsum]</span></td></tr>
			</table>
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			AMPA receptors are the major excitatory neurotransmitter receptors in the CNS and are involved in numerous neurological disorders. An agonist-binding site is present in each of four subunits that form a functional channel. Binding consists of three steps: docking of agonist to the bi-lobed ligand binding domain (LBD), closure of the LBD, and increased stability of the closed-lobe conformation through interlobe hydrogen bonding. We describe GluA3 single channel currents activated by nitrowillardiine (NO(2)W) and chlorowillardiine (ClW) in the presence of cyclothiazide, in conjunction with crystal structures of GluA2 and GluA3 LBDs bound to fluorowillardiine (FW), ClW, and NO(2)W. When bound to NO(2)W or ClW, the GluA3 channel opens to three conductance levels with comparable open probabilities and displays modal behavior similar to that obtained with glutamate and FW as agonists (Poon et al., 2010). At lower concentrations, ClW evoked an alternate kinetic behavior, consisting of high open probability in lower conductance states. The structure of ClW bound to GluA3 LBD exhibits a unique partially open hydrogen bonding structure that may be associated with these alternative kinetics. NO(2)W evoked longer open times than seen for other agonists in high and very high modes. The structure of GluA2 LBD bound to NO2W exhibits fully closed lobes with additional interlobe interactions mediated by the nitro group. Beyond differences in efficacy between full and partial agonists, the complexities of the single channel behavior of AMPA receptors may also be associated with small interactions that modify the stability of various degrees of closure.

	~~{{STRUCTURE_3rtf\| PDB=3rtf \| SCENE= }}~~		Mechanisms of Modal Activation of GluA3 Receptors.,Poon K, Ahmed AH, Nowak LM, Oswald RE Mol Pharmacol. 2011 Apr 4. PMID:21464198<ref>PMID:21464198</ref>

	~~===Chlorowillardiine bound to~~ the ~~ligand binding domain of GluA2===~~		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
			</div>
	~~{{ABSTRACT_PUBMED_21464198}}~~

	~~==About this Structure==~~
	~~[[3rtf]] is a 3 chain structure with sequence from [http://en~~.~~wikipedia~~.~~org/wiki/Rattus_norvegicus Rattus norvegicus]~~. ~~Full crystallographic information is available from [http:~~/~~/oca.weizmann.ac.il/oca-bin/ocashort?id=3RTF OCA].~~

	==See Also==		==See Also==
	*[[Ionotropic Glutamate Receptors\|Ionotropic Glutamate Receptors]]		*[[Ionotropic Glutamate Receptors\|Ionotropic Glutamate Receptors]]
			== References ==
	==~~Reference~~==		<references/>
	<~~ref group="xtra">PMID:021464198<~~/~~ref~~><~~references group="xtra"~~/>		__TOC__
			</StructureSection>
	[[Category: Rattus norvegicus]]		[[Category: Rattus norvegicus]]
	[[Category: Ahmed, A H.]]		[[Category: Ahmed, A H]]
	[[Category: Oswald, R E.]]		[[Category: Oswald, R E]]
	[[Category: Ampa receptor]]		[[Category: Ampa receptor]]
	[[Category: Glur2]]		[[Category: Glur2]]

OCA at 20:35, 20 October 2012

2012-10-20T20:35:38Z

← Older revision		Revision as of 20:35, 20 October 2012
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	==About this Structure==		==About this Structure==
	[[3rtf]] is a 3 chain structure ~~of [[Ionotropic Glutamate Receptors]]~~ with sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RTF OCA].		[[3rtf]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RTF OCA].

	==See Also==		==See Also==

OCA at 10:59, 27 July 2012

2012-07-27T10:59:18Z

← Older revision		Revision as of 10:59, 27 July 2012
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	[[Image:3rtf.png\|left\|200px]]		[[Image:3rtf.png\|left\|200px]]

	~~<!--~~
	~~The line below this paragraph, containing "STRUCTURE_3rtf", 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_3rtf\| PDB=3rtf \| SCENE= }}		{{STRUCTURE_3rtf\| PDB=3rtf \| SCENE= }}

	===Chlorowillardiine bound to the ligand binding domain of GluA2===		===Chlorowillardiine bound to the ligand binding domain of GluA2===


	~~<!--~~
	~~The line below this paragraph, {{ABSTRACT_PUBMED_21464198}}, adds the Publication Abstract to the page~~
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	==See Also==		==See Also==
	*[[Ionotropic Glutamate Receptors]]		*[[Ionotropic Glutamate Receptors\|Ionotropic Glutamate Receptors]]

	==Reference==		==Reference==

OCA at 18:03, 6 July 2011

2011-07-06T18:03:29Z

← Older revision		Revision as of 18:03, 6 July 2011
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	[[Image:3rtf.~~jpg~~\|left\|200px]]		[[Image:3rtf.png\|left\|200px]]

	<!--		<!--
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	==About this Structure==		==About this Structure==
	[[3rtf]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RTF OCA].		[[3rtf]] is a 3 chain structure of [[Ionotropic Glutamate Receptors]] with sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RTF OCA].

			==See Also==
			*[[Ionotropic Glutamate Receptors]]

	==Reference==		==Reference==
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	[[Category: Ahmed, A H.]]		[[Category: Ahmed, A H.]]
	[[Category: Oswald, R E.]]		[[Category: Oswald, R E.]]
			[[Category: Ampa receptor]]
			[[Category: Glur2]]
			[[Category: Glutamate receptor]]
			[[Category: Neurotransmitter receptor]]
			[[Category: S1s2]]
			[[Category: Transport protein]]