1mxv - Revision history

OCA at 04:44, 17 October 2024

2024-10-17T04:44:08Z

← Older revision		Revision as of 04:44, 17 October 2024
Line 15:		Line 15:
	<jmolCheckbox>		<jmolCheckbox>
	<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/mx/1mxv_consurf.spt"</scriptWhenChecked>		<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/mx/1mxv_consurf.spt"</scriptWhenChecked>
	<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/~~initialview01~~.spt</scriptWhenUnchecked>		<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
	<text>to colour the structure by Evolutionary Conservation</text>		<text>to colour the structure by Evolutionary Conservation</text>
	</jmolCheckbox>		</jmolCheckbox>
	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1mxv ConSurf].		</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1mxv ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			Numerous naturally occurring and synthetic alpha-amino acids act as agonists on (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazole) propionic acid (AMPA) receptors but nevertheless display significant differences in their functional properties and modes of interaction. The 5-substituted willardiines are a series of compounds that exhibit a range of affinities, act as partial agonists, and give rise to intermediate levels of activation and desensitization. However, the molecular basis for the activities of 5-substituted willardiines has not been conclusively elaborated at the level of atomic resolution. Here we provide insight into the molecular basis of the potency and efficacy elicited by the 5-substituted willardiines on the basis of cocrystal structures with the GluR2 ligand-binding core. We also show that the crystallized ligand-binding core has an affinity for agonists similar to the ligand-binding core in solution. Analysis of multiple crystal lattices suggests modes by which the ligand-binding core dimers interact in the tetrameric receptor. These studies further our understanding of how subtle differences in the structures of agonists are correlated to changes in the conformation of residues and water molecules in the immediate binding pocket and to the degree of domain closure.

			Probing the function, conformational plasticity, and dimer-dimer contacts of the GluR2 ligand-binding core: studies of 5-substituted willardiines and GluR2 S1S2 in the crystal.,Jin R, Gouaux E Biochemistry. 2003 May 13;42(18):5201-13. PMID:12731861<ref>PMID:12731861</ref>

			From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
			</div>
			<div class="pdbe-citations 1mxv" style="background-color:#fffaf0;"></div>

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

OCA at 06:08, 3 April 2024

2024-04-03T06:08:05Z

← Older revision		Revision as of 06:08, 3 April 2024
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	<StructureSection load='1mxv' size='340' side='right'caption='[[1mxv]], [[Resolution\|resolution]] 1.95Å' scene=''>		<StructureSection load='1mxv' size='340' side='right'caption='[[1mxv]], [[Resolution\|resolution]] 1.95Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[1mxv]] 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=1MXV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1MXV FirstGlance]. <br>		<table><tr><td colspan='2'>[[1mxv]] 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=1MXV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1MXV FirstGlance]. <br>
	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat" id="~~ligandDat~~">~~<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]] 1.95Å</td></tr>
	<tr id='~~related~~'><td class="sblockLbl"><b>[[~~Related_structure~~\|~~Related~~:]]</b></td><td class="sblockDat"><~~div style~~='~~overflow~~: ~~auto; max-height: 3em;~~'>~~[[1mqh\|1mqh]], [[1ftm\|1ftm]], [[1mxu\|1mxu]], [[1mxw\|1mxw]], [[1mxx\|1mxx]], [[1mxy\|1mxy]], [[1mxz\|1mxz]], [[1my0\|1my0]], [[1my1\|1my1]], [[1my2\|1my2]], [[1my3\|1my3]]~~</~~div~~></td></tr>		<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></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=1mxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mxv OCA], [https://pdbe.org/1mxv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1mxv RCSB], [https://www.ebi.ac.uk/pdbsum/1mxv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1mxv 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=1mxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mxv OCA], [https://pdbe.org/1mxv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1mxv RCSB], [https://www.ebi.ac.uk/pdbsum/1mxv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1mxv 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>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
Line 20:		Line 20:
	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1mxv ConSurf].		</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1mxv ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
	~~<div style="background-color:#fffaf0;">~~
	~~== Publication Abstract from PubMed ==~~
	Numerous naturally occurring and synthetic alpha-amino acids act as agonists on (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazole) propionic acid (AMPA) receptors but nevertheless display significant differences in their functional properties and modes of interaction. The 5-substituted willardiines are a series of compounds that exhibit a range of affinities, act as partial agonists, and give rise to intermediate levels of activation and desensitization. However, the molecular basis for the activities of 5-substituted willardiines has not been conclusively elaborated at the level of atomic resolution. Here we provide insight into the molecular basis of the potency and efficacy elicited by the 5-substituted willardiines on the basis of cocrystal structures with the GluR2 ligand-binding core. We also show that the crystallized ligand-binding core has an affinity for agonists similar to the ligand-binding core in solution. Analysis of multiple crystal lattices suggests modes by which the ligand-binding core dimers interact in the tetrameric receptor. These studies further our understanding of how subtle differences in the structures of agonists are correlated to changes in the conformation of residues and water molecules in the immediate binding pocket and to the degree of domain closure.

	Probing the function, conformational plasticity, and dimer-dimer contacts of the GluR2 ligand-binding core: studies of 5-substituted willardiines and GluR2 S1S2 in the crystal.,Jin R, Gouaux E Biochemistry. 2003 May 13;42(18):5201-13. PMID:12731861<ref>PMID:12731861</ref>

	~~From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>~~
	~~</div>~~
	~~<div class="pdbe-citations 1mxv" style="background-color:#fffaf0;"></div>~~

	==See Also==		==See Also==
Line 36:		Line 27:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	~~[[Category: Buffalo rat]]~~
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: ~~Gouaux, E~~]]		[[Category: Rattus norvegicus]]
	[[Category: ~~Jin, R~~]]		[[Category: Gouaux E]]
	[[Category: ~~Ampa]]~~		[[Category: Jin R]]
	~~[[Category: Bromo-willardiine]]~~
	~~[[Category: Crystal titration]]~~
	~~[[Category: Glur2]]~~
	~~[[Category: Ionotropic glutamate receptor]]~~
	~~[[Category: Ligand binding core]]~~
	~~[[Category: Membrane protein]]~~
	~~[[Category: Partial agonist]]~~
	~~[[Category: S1s2~~]]

OCA at 09:53, 26 May 2021

2021-05-26T09:53:21Z

← Older revision		Revision as of 09:53, 26 May 2021
Line 3:		Line 3:
	<StructureSection load='1mxv' size='340' side='right'caption='[[1mxv]], [[Resolution\|resolution]] 1.95Å' scene=''>		<StructureSection load='1mxv' size='340' side='right'caption='[[1mxv]], [[Resolution\|resolution]] 1.95Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[1mxv]] 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=1MXV OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=1MXV FirstGlance]. <br>		<table><tr><td colspan='2'>[[1mxv]] 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=1MXV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1MXV FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><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=ZN:ZINC+ION'>ZN</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1mqh\|1mqh]], [[1ftm\|1ftm]], [[1mxu\|1mxu]], [[1mxw\|1mxw]], [[1mxx\|1mxx]], [[1mxy\|1mxy]], [[1mxz\|1mxz]], [[1my0\|1my0]], [[1my1\|1my1]], [[1my2\|1my2]], [[1my3\|1my3]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1mqh\|1mqh]], [[1ftm\|1ftm]], [[1mxu\|1mxu]], [[1mxw\|1mxw]], [[1mxx\|1mxx]], [[1mxy\|1mxy]], [[1mxz\|1mxz]], [[1my0\|1my0]], [[1my1\|1my1]], [[1my2\|1my2]], [[1my3\|1my3]]</div></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=1mxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mxv OCA], [~~http~~://pdbe.org/1mxv PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=1mxv RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/1mxv PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=1mxv 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=1mxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mxv OCA], [https://pdbe.org/1mxv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1mxv RCSB], [https://www.ebi.ac.uk/pdbsum/1mxv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1mxv 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>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]

OCA at 07:46, 21 August 2019

2019-08-21T07:46:06Z

← Older revision		Revision as of 07:46, 21 August 2019
Line 1:		Line 1:

	==crystal titration experiments (AMPA co-crystals soaked in 10 mM BrW)==		==crystal titration experiments (AMPA co-crystals soaked in 10 mM BrW)==
	<StructureSection load='1mxv' size='340' side='right' caption='[[1mxv]], [[Resolution\|resolution]] 1.95Å' scene=''>		<StructureSection load='1mxv' size='340' side='right'caption='[[1mxv]], [[Resolution\|resolution]] 1.95Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[1mxv]] 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=1MXV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1MXV FirstGlance]. <br>		<table><tr><td colspan='2'>[[1mxv]] 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=1MXV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1MXV FirstGlance]. <br>
Line 14:		Line 14:
	Check<jmol>		Check<jmol>
	<jmolCheckbox>		<jmolCheckbox>
	<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/mx/1mxv_consurf.spt"</scriptWhenChecked>		<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/mx/1mxv_consurf.spt"</scriptWhenChecked>
	<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>		<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
	<text>to colour the structure by Evolutionary Conservation</text>		<text>to colour the structure by Evolutionary Conservation</text>
Line 29:		Line 29:
	</div>		</div>
	<div class="pdbe-citations 1mxv" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 1mxv" style="background-color:#fffaf0;"></div>

			==See Also==
			*[[Glutamate receptor 3D structures\|Glutamate receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
Line 34:		Line 37:
	</StructureSection>		</StructureSection>
	[[Category: Buffalo rat]]		[[Category: Buffalo rat]]
			[[Category: Large Structures]]
	[[Category: Gouaux, E]]		[[Category: Gouaux, E]]
	[[Category: Jin, R]]		[[Category: Jin, R]]

OCA at 21:23, 15 November 2017

2017-11-15T21:23:44Z

← Older revision		Revision as of 21:23, 15 November 2017
Line 1:		Line 1:

	==crystal titration experiments (AMPA co-crystals soaked in 10 mM BrW)==		==crystal titration experiments (AMPA co-crystals soaked in 10 mM BrW)==
	<StructureSection load='1mxv' size='340' side='right' caption='[[1mxv]], [[Resolution\|resolution]] 1.95Å' scene=''>		<StructureSection load='1mxv' size='340' side='right' caption='[[1mxv]], [[Resolution\|resolution]] 1.95Å' scene=''>
Line 5:		Line 6:
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><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=ZN:ZINC+ION'>ZN</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1mqh\|1mqh]], [[1ftm\|1ftm]], [[1mxu\|1mxu]], [[1mxw\|1mxw]], [[1mxx\|1mxx]], [[1mxy\|1mxy]], [[1mxz\|1mxz]], [[1my0\|1my0]], [[1my1\|1my1]], [[1my2\|1my2]], [[1my3\|1my3]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1mqh\|1mqh]], [[1ftm\|1ftm]], [[1mxu\|1mxu]], [[1mxw\|1mxw]], [[1mxx\|1mxx]], [[1mxy\|1mxy]], [[1mxz\|1mxz]], [[1my0\|1my0]], [[1my1\|1my1]], [[1my2\|1my2]], [[1my3\|1my3]]</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=1mxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mxv OCA], [http://pdbe.org/1mxv PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1mxv RCSB], [http://www.ebi.ac.uk/pdbsum/1mxv 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=1mxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mxv OCA], [http://pdbe.org/1mxv PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1mxv RCSB], [http://www.ebi.ac.uk/pdbsum/1mxv PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=1mxv ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 28:		Line 29:
	</div>		</div>
	<div class="pdbe-citations 1mxv" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 1mxv" style="background-color:#fffaf0;"></div>

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

OCA at 08:33, 9 February 2016

2016-02-09T08:33:36Z

← Older revision		Revision as of 08:33, 9 February 2016
Line 17:		Line 17:
	<text>to colour the structure by Evolutionary Conservation</text>		<text>to colour the structure by Evolutionary Conservation</text>
	</jmolCheckbox>		</jmolCheckbox>
	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/~~chain_selection~~.php?pdb_ID=~~2ata~~ ConSurf].		</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1mxv ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">

OCA at 20:29, 10 September 2015

2015-09-10T20:29:35Z

← Older revision		Revision as of 20:29, 10 September 2015
Line 2:		Line 2:
	<StructureSection load='1mxv' size='340' side='right' caption='[[1mxv]], [[Resolution\|resolution]] 1.95Å' scene=''>		<StructureSection load='1mxv' size='340' side='right' caption='[[1mxv]], [[Resolution\|resolution]] 1.95Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[1mxv]] 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=1MXV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1MXV FirstGlance]. <br>		<table><tr><td colspan='2'>[[1mxv]] 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=1MXV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1MXV FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><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=ZN:ZINC+ION'>ZN</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1mqh\|1mqh]], [[1ftm\|1ftm]], [[1mxu\|1mxu]], [[1mxw\|1mxw]], [[1mxx\|1mxx]], [[1mxy\|1mxy]], [[1mxz\|1mxz]], [[1my0\|1my0]], [[1my1\|1my1]], [[1my2\|1my2]], [[1my3\|1my3]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1mqh\|1mqh]], [[1ftm\|1ftm]], [[1mxu\|1mxu]], [[1mxw\|1mxw]], [[1mxx\|1mxx]], [[1mxy\|1mxy]], [[1mxz\|1mxz]], [[1my0\|1my0]], [[1my1\|1my1]], [[1my2\|1my2]], [[1my3\|1my3]]</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=1mxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mxv OCA], [http://www.rcsb.org/pdb/explore.do?structureId=1mxv RCSB], [http://www.ebi.ac.uk/pdbsum/1mxv 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=1mxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mxv OCA], [http://pdbe.org/1mxv PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1mxv RCSB], [http://www.ebi.ac.uk/pdbsum/1mxv PDBsum]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 27:		Line 27:
	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 1mxv" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 34:		Line 35:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Rattus norvegicus~~]]		[[Category: Buffalo rat]]
	[[Category: Gouaux, E]]		[[Category: Gouaux, E]]
	[[Category: Jin, R]]		[[Category: Jin, R]]

OCA at 05:44, 25 December 2014

2014-12-25T05:44:51Z

← Older revision		Revision as of 05:44, 25 December 2014
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[1mxv]] 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=1MXV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1MXV FirstGlance]. <br>		<table><tr><td colspan='2'>[[1mxv]] 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=1MXV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1MXV FirstGlance]. <br>
	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ZN:ZINC+ION'>ZN</scene><br>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1mqh\|1mqh]], [[1ftm\|1ftm]], [[1mxu\|1mxu]], [[1mxw\|1mxw]], [[1mxx\|1mxx]], [[1mxy\|1mxy]], [[1mxz\|1mxz]], [[1my0\|1my0]], [[1my1\|1my1]], [[1my2\|1my2]], [[1my3\|1my3]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1mqh\|1mqh]], [[1ftm\|1ftm]], [[1mxu\|1mxu]], [[1mxw\|1mxw]], [[1mxx\|1mxx]], [[1mxy\|1mxy]], [[1mxz\|1mxz]], [[1my0\|1my0]], [[1my1\|1my1]], [[1my2\|1my2]], [[1my3\|1my3]]</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=1mxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mxv OCA], [http://www.rcsb.org/pdb/explore.do?structureId=1mxv RCSB], [http://www.ebi.ac.uk/pdbsum/1mxv 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=1mxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mxv OCA], [http://www.rcsb.org/pdb/explore.do?structureId=1mxv RCSB], [http://www.ebi.ac.uk/pdbsum/1mxv 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>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
Line 33:		Line 35:
	</StructureSection>		</StructureSection>
	[[Category: Rattus norvegicus]]		[[Category: Rattus norvegicus]]
	[[Category: Gouaux, E.]]		[[Category: Gouaux, E]]
	[[Category: Jin, R.]]		[[Category: Jin, R]]
	[[Category: Ampa]]		[[Category: Ampa]]
	[[Category: Bromo-willardiine]]		[[Category: Bromo-willardiine]]

OCA at 16:16, 28 September 2014

2014-09-28T16:16:27Z

← Older revision		Revision as of 16:16, 28 September 2014
Line 1:		Line 1:
	[[Image:~~1mxv~~.~~png~~\|~~left~~\|~~200px~~]]		==crystal titration experiments (AMPA co-crystals soaked in 10 mM BrW)==
			<StructureSection load='1mxv' size='340' side='right' caption='[[1mxv]], [[Resolution\|resolution]] 1.95Å' scene=''>
			== Structural highlights ==
			<table><tr><td colspan='2'>[[1mxv]] 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=1MXV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1MXV FirstGlance]. <br>
			</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ZN:ZINC+ION'>ZN</scene><br>
			<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1mqh\|1mqh]], [[1ftm\|1ftm]], [[1mxu\|1mxu]], [[1mxw\|1mxw]], [[1mxx\|1mxx]], [[1mxy\|1mxy]], [[1mxz\|1mxz]], [[1my0\|1my0]], [[1my1\|1my1]], [[1my2\|1my2]], [[1my3\|1my3]]</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=1mxv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mxv OCA], [http://www.rcsb.org/pdb/explore.do?structureId=1mxv RCSB], [http://www.ebi.ac.uk/pdbsum/1mxv PDBsum]</span></td></tr>
			<table>
			== Evolutionary Conservation ==
			[[Image:Consurf_key_small.gif\|200px\|right]]
			Check<jmol>
			<jmolCheckbox>
			<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/mx/1mxv_consurf.spt"</scriptWhenChecked>
			<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
			<text>to colour the structure by Evolutionary Conservation</text>
			</jmolCheckbox>
			</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/chain_selection.php?pdb_ID=2ata ConSurf].
			<div style="clear:both"></div>
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			Numerous naturally occurring and synthetic alpha-amino acids act as agonists on (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazole) propionic acid (AMPA) receptors but nevertheless display significant differences in their functional properties and modes of interaction. The 5-substituted willardiines are a series of compounds that exhibit a range of affinities, act as partial agonists, and give rise to intermediate levels of activation and desensitization. However, the molecular basis for the activities of 5-substituted willardiines has not been conclusively elaborated at the level of atomic resolution. Here we provide insight into the molecular basis of the potency and efficacy elicited by the 5-substituted willardiines on the basis of cocrystal structures with the GluR2 ligand-binding core. We also show that the crystallized ligand-binding core has an affinity for agonists similar to the ligand-binding core in solution. Analysis of multiple crystal lattices suggests modes by which the ligand-binding core dimers interact in the tetrameric receptor. These studies further our understanding of how subtle differences in the structures of agonists are correlated to changes in the conformation of residues and water molecules in the immediate binding pocket and to the degree of domain closure.

	~~{{STRUCTURE_1mxv\| PDB=1mxv \| SCENE= }}~~		Probing the function, conformational plasticity, and dimer-dimer contacts of the GluR2 ligand-binding core: studies of 5-substituted willardiines and GluR2 S1S2 in the crystal.,Jin R, Gouaux E Biochemistry. 2003 May 13;42(18):5201-13. PMID:12731861<ref>PMID:12731861</ref>

	~~===crystal titration experiments (AMPA co-crystals soaked in 10 mM BrW)===~~		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
			</div>
	~~{{ABSTRACT_PUBMED_12731861}}~~

	~~==About this Structure==~~
	~~[[1mxv]] 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=1MXV OCA].~~

	==See Also==		==See Also==
	*[[Ionotropic Glutamate Receptors\|Ionotropic Glutamate Receptors]]		*[[Ionotropic Glutamate Receptors\|Ionotropic Glutamate Receptors]]
			== References ==
	==~~Reference~~==		<references/>
	<~~ref group="xtra">PMID:012731861<~~/~~ref~~><~~references group="xtra"~~/>		__TOC__
			</StructureSection>
	[[Category: Rattus norvegicus]]		[[Category: Rattus norvegicus]]
	[[Category: Gouaux, E.]]		[[Category: Gouaux, E.]]

OCA at 13:17, 20 October 2012

2012-10-20T13:17:18Z

← Older revision		Revision as of 13:17, 20 October 2012
Line 8:		Line 8:

	==About this Structure==		==About this Structure==
	[[1mxv]] 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=1MXV OCA].		[[1mxv]] 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=1MXV OCA].

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