3pmx - Revision history

OCA at 02:16, 21 November 2024

2024-11-21T02:16:53Z

← Older revision		Revision as of 02:16, 21 November 2024
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	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3pmx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmx OCA], [https://pdbe.org/3pmx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3pmx RCSB], [https://www.ebi.ac.uk/pdbsum/3pmx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3pmx 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=3pmx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmx OCA], [https://pdbe.org/3pmx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3pmx RCSB], [https://www.ebi.ac.uk/pdbsum/3pmx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3pmx ProSAT]</span></td></tr>
	</table>		</table>
	== ~~Function~~ ==		<div style="background-color:#fffaf0;">
	[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~~>		== Publication Abstract from PubMed ==
			Starting from compound 1, we utilized biostructural data to successfully evolve an existing series into a new chemotype with a promising overall profile, exemplified by 19.

			Structure based evolution of a novel series of positive modulators of the AMPA receptor.,Jamieson C, Maclean JK, Brown CI, Campbell RA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L Bioorg Med Chem Lett. 2011 Jan 15;21(2):805-11. Epub 2010 Nov 25. PMID:21190850<ref>PMID:21190850</ref>

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

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

OCA at 13:32, 1 March 2024

2024-03-01T13:32:36Z

← Older revision		Revision as of 13:32, 1 March 2024
Line 3:		Line 3:
	<StructureSection load='3pmx' size='340' side='right'caption='[[3pmx]], [[Resolution\|resolution]] 1.87Å' scene=''>		<StructureSection load='3pmx' size='340' side='right'caption='[[3pmx]], [[Resolution\|resolution]] 1.87Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3pmx]] is a 1 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=3PMX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PMX FirstGlance]. <br>		<table><tr><td colspan='2'>[[3pmx]] is a 1 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=3PMX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PMX FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=808:N-[(2S)-5-{[5-(TRIFLUOROMETHYL)FURAN-2-YL]METHYL}-2,3-DIHYDRO-1H-INDEN-2-YL]PROPANE-2-SULFONAMIDE'>808</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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]] 1.87Å</td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[3o28\|3o28]], [[3o29\|3o29]], [[3o2a\|3o2a]], [[3o6g\|3o6g]], [[3o6h\|3o6h]], [[3o6i\|3o6i]], [[3pmv\|3pmv]], [[3pmw\|3pmw]]</div></td></tr>		<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=808:N-[(2S)-5-{[5-(TRIFLUOROMETHYL)FURAN-2-YL]METHYL}-2,3-DIHYDRO-1H-INDEN-2-YL]PROPANE-2-SULFONAMIDE'>808</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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=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=3pmx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmx OCA], [https://pdbe.org/3pmx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3pmx RCSB], [https://www.ebi.ac.uk/pdbsum/3pmx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3pmx 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=3pmx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmx OCA], [https://pdbe.org/3pmx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3pmx RCSB], [https://www.ebi.ac.uk/pdbsum/3pmx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3pmx 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 ==~~
	~~Starting from compound 1, we utilized biostructural data to successfully evolve an existing series into a new chemotype with a promising overall profile, exemplified by 19.~~

	Structure based evolution of a novel series of positive modulators of the AMPA receptor.,Jamieson C, Maclean JK, Brown CI, Campbell RA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L Bioorg Med Chem Lett. 2011 Jan 15;21(2):805-11. Epub 2010 Nov 25. PMID:21190850<ref>PMID:21190850</ref>

	~~From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>~~
	~~</div>~~
	~~<div class="pdbe-citations 3pmx" 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: Brown~~, C I~~]]		[[Category: Rattus norvegicus]]
	[[Category: Campbell~~, R A~~]]		[[Category: Brown CI]]
	[[Category: Gillen~~, K J~~]]		[[Category: Campbell RA]]
	[[Category: Gillespie, J]]		[[Category: Gillen KJ]]
	[[Category: Jamieson, C]]		[[Category: Gillespie J]]
	[[Category: Kazemier, B]]		[[Category: Jamieson C]]
	[[Category: Kiczun, M]]		[[Category: Kazemier B]]
	[[Category: Lamont, Y]]		[[Category: Kiczun M]]
	[[Category: Lyons~~, A J~~]]		[[Category: Lamont Y]]
	[[Category: Maclean~~, J K.F~~]]		[[Category: Lyons AJ]]
	[[Category: Moir~~, E M~~]]		[[Category: Maclean JKF]]
	[[Category: Morrow~~, J A~~]]		[[Category: Moir EM]]
	[[Category: Pantling, J]]		[[Category: Morrow JA]]
	[[Category: Rankovic, Z]]		[[Category: Pantling J]]
	[[Category: Smith, L]]		[[Category: Rankovic Z]]
	~~[[Category: Chimera protein]]~~		[[Category: Smith L]]
	~~[[Category: Fusion protein]]~~
	~~[[Category: Membrane protein]]~~
	~~[[Category: Transport protein~~]]

OCA at 08:46, 25 May 2022

2022-05-25T08:46:21Z

← Older revision		Revision as of 08:46, 25 May 2022
Line 1:		Line 1:

	==Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator==		==Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator==
	<StructureSection load='3pmx' size='340' side='right' caption='[[3pmx]], [[Resolution\|resolution]] 1.87Å' scene=''>		<StructureSection load='3pmx' size='340' side='right'caption='[[3pmx]], [[Resolution\|resolution]] 1.87Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3pmx]] is a 1 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=3PMX OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3PMX FirstGlance]. <br>		<table><tr><td colspan='2'>[[3pmx]] is a 1 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=3PMX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PMX FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=808:N-[(2S)-5-{[5-(TRIFLUOROMETHYL)FURAN-2-YL]METHYL}-2,3-DIHYDRO-1H-INDEN-2-YL]PROPANE-2-SULFONAMIDE'>808</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=808:N-[(2S)-5-{[5-(TRIFLUOROMETHYL)FURAN-2-YL]METHYL}-2,3-DIHYDRO-1H-INDEN-2-YL]PROPANE-2-SULFONAMIDE'>808</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3o28\|3o28]], [[3o29\|3o29]], [[3o2a\|3o2a]], [[3o6g\|3o6g]], [[3o6h\|3o6h]], [[3o6i\|3o6i]], [[3pmv\|3pmv]], [[3pmw\|3pmw]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[3o28\|3o28]], [[3o29\|3o29]], [[3o2a\|3o2a]], [[3o6g\|3o6g]], [[3o6h\|3o6h]], [[3o6i\|3o6i]], [[3pmv\|3pmv]], [[3pmw\|3pmw]]</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=10116 Buffalo rat])</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=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=3pmx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmx OCA], [~~http~~://pdbe.org/3pmx PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3pmx RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3pmx PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=3pmx 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=3pmx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmx OCA], [https://pdbe.org/3pmx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3pmx RCSB], [https://www.ebi.ac.uk/pdbsum/3pmx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3pmx 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 22:		Line 22:

	==See Also==		==See Also==
	*[[~~Ionotropic~~ Glutamate ~~Receptors~~\|~~Ionotropic~~ Glutamate ~~Receptors~~]]		*[[Glutamate receptor 3D structures\|Glutamate receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
Line 28:		Line 28:
	</StructureSection>		</StructureSection>
	[[Category: Buffalo rat]]		[[Category: Buffalo rat]]
			[[Category: Large Structures]]
	[[Category: Brown, C I]]		[[Category: Brown, C I]]
	[[Category: Campbell, R A]]		[[Category: Campbell, R A]]

OCA at 23:25, 4 August 2016

2016-08-04T23:25:07Z

← Older revision		Revision as of 23:25, 4 August 2016
Line 1:		Line 1:

	==Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator==		==Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator==
	<StructureSection load='3pmx' size='340' side='right' caption='[[3pmx]], [[Resolution\|resolution]] 1.87Å' scene=''>		<StructureSection load='3pmx' size='340' side='right' caption='[[3pmx]], [[Resolution\|resolution]] 1.87Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3pmx]] is a 1 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=3PMX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3PMX FirstGlance]. <br>		<table><tr><td colspan='2'>[[3pmx]] is a 1 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=3PMX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3PMX FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=808:N-[(2S)-5-{[5-(TRIFLUOROMETHYL)FURAN-2-YL]METHYL}-2,3-DIHYDRO-1H-INDEN-2-YL]PROPANE-2-SULFONAMIDE'>808</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=808:N-[(2S)-5-{[5-(TRIFLUOROMETHYL)FURAN-2-YL]METHYL}-2,3-DIHYDRO-1H-INDEN-2-YL]PROPANE-2-SULFONAMIDE'>808</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3o28\|3o28]], [[3o29\|3o29]], [[3o2a\|3o2a]], [[3o6g\|3o6g]], [[3o6h\|3o6h]], [[3o6i\|3o6i]], [[3pmv\|3pmv]], [[3pmw\|3pmw]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3o28\|3o28]], [[3o29\|3o29]], [[3o2a\|3o2a]], [[3o6g\|3o6g]], [[3o6h\|3o6h]], [[3o6i\|3o6i]], [[3pmv\|3pmv]], [[3pmw\|3pmw]]</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=10116 ~~Rattus norvegicus~~])</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=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=3pmx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmx OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3pmx RCSB], [http://www.ebi.ac.uk/pdbsum/3pmx 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=3pmx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmx OCA], [http://pdbe.org/3pmx PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3pmx RCSB], [http://www.ebi.ac.uk/pdbsum/3pmx PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3pmx 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 3pmx" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 25:		Line 27:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Rattus norvegicus~~]]		[[Category: Buffalo rat]]
	[[Category: Brown, C I]]		[[Category: Brown, C I]]
	[[Category: Campbell, R A]]		[[Category: Campbell, R A]]

OCA at 20:40, 24 December 2014

2014-12-24T20:40:01Z

← Older revision		Revision as of 20:40, 24 December 2014
Line 8:		Line 8:
	<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=3pmx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmx OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3pmx RCSB], [http://www.ebi.ac.uk/pdbsum/3pmx 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=3pmx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmx OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3pmx RCSB], [http://www.ebi.ac.uk/pdbsum/3pmx 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 13:19, 9 December 2014

2014-12-09T13:19:22Z

← Older revision		Revision as of 13:19, 9 December 2014
Line 1:		Line 1:
	[[~~Image~~:~~3pmx~~.~~png~~\|~~left~~\|~~200px~~]]		==Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator==
			<StructureSection load='3pmx' size='340' side='right' caption='[[3pmx]], [[Resolution\|resolution]] 1.87Å' scene=''>
			== Structural highlights ==
			<table><tr><td colspan='2'>[[3pmx]] is a 1 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=3PMX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3PMX FirstGlance]. <br>
			</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=808:N-[(2S)-5-{[5-(TRIFLUOROMETHYL)FURAN-2-YL]METHYL}-2,3-DIHYDRO-1H-INDEN-2-YL]PROPANE-2-SULFONAMIDE'>808</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GLU:GLUTAMIC+ACID'>GLU</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
			<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3o28\|3o28]], [[3o29\|3o29]], [[3o2a\|3o2a]], [[3o6g\|3o6g]], [[3o6h\|3o6h]], [[3o6i\|3o6i]], [[3pmv\|3pmv]], [[3pmw\|3pmw]]</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=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=3pmx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pmx OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3pmx RCSB], [http://www.ebi.ac.uk/pdbsum/3pmx PDBsum]</span></td></tr>
			</table>
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			Starting from compound 1, we utilized biostructural data to successfully evolve an existing series into a new chemotype with a promising overall profile, exemplified by 19.

	~~{{STRUCTURE_3pmx\| PDB=3pmx \| SCENE= }}~~		Structure based evolution of a novel series of positive modulators of the AMPA receptor.,Jamieson C, Maclean JK, Brown CI, Campbell RA, Gillen KJ, Gillespie J, Kazemier B, Kiczun M, Lamont Y, Lyons AJ, Moir EM, Morrow JA, Pantling J, Rankovic Z, Smith L Bioorg Med Chem Lett. 2011 Jan 15;21(2):805-11. Epub 2010 Nov 25. PMID:21190850<ref>PMID:21190850</ref>

	~~===Ligand-binding domain~~ of ~~GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator===~~		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
			</div>
	~~{{ABSTRACT_PUBMED_21190850}}~~

	~~==About this Structure==~~
	~~[[3pmx]] is a 1 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=3PMX OCA].~~

	==See Also==		==See Also==
	*[[Ionotropic Glutamate Receptors\|Ionotropic Glutamate Receptors]]		*[[Ionotropic Glutamate Receptors\|Ionotropic Glutamate Receptors]]
			== References ==
	==~~Reference~~==		<references/>
	<~~ref group="xtra">PMID:021190850<~~/~~ref~~><~~references group="xtra"~~/>		__TOC__
			</StructureSection>
	[[Category: Rattus norvegicus]]		[[Category: Rattus norvegicus]]
	[[Category: Brown, C I.]]		[[Category: Brown, C I]]
	[[Category: Campbell, R A.]]		[[Category: Campbell, R A]]
	[[Category: Gillen, K J.]]		[[Category: Gillen, K J]]
	[[Category: Gillespie, J.]]		[[Category: Gillespie, J]]
	[[Category: Jamieson, C.]]		[[Category: Jamieson, C]]
	[[Category: Kazemier, B.]]		[[Category: Kazemier, B]]
	[[Category: Kiczun, M.]]		[[Category: Kiczun, M]]
	[[Category: Lamont, Y.]]		[[Category: Lamont, Y]]
	[[Category: Lyons, A J.]]		[[Category: Lyons, A J]]
	[[Category: Maclean, J K.F.]]		[[Category: Maclean, J K.F]]
	[[Category: Moir, E M.]]		[[Category: Moir, E M]]
	[[Category: Morrow, J A.]]		[[Category: Morrow, J A]]
	[[Category: Pantling, J.]]		[[Category: Pantling, J]]
	[[Category: Rankovic, Z.]]		[[Category: Rankovic, Z]]
	[[Category: Smith, L.]]		[[Category: Smith, L]]
	[[Category: Chimera protein]]		[[Category: Chimera protein]]
	[[Category: Fusion protein]]		[[Category: Fusion protein]]
	[[Category: Membrane protein]]		[[Category: Membrane protein]]
	[[Category: Transport protein]]		[[Category: Transport protein]]

OCA at 08:55, 20 October 2012

2012-10-20T08:55:58Z

← Older revision		Revision as of 08:55, 20 October 2012
Line 8:		Line 8:

	==About this Structure==		==About this Structure==
	[[3pmx]] is a 1 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=3PMX OCA].		[[3pmx]] is a 1 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=3PMX OCA].

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

OCA at 21:14, 25 July 2012

2012-07-25T21:14:20Z

← Older revision		Revision as of 21:14, 25 July 2012
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	[[Image:3pmx.png\|left\|200px]]		[[Image:3pmx.png\|left\|200px]]

	~~<!--~~
	~~The line below this paragraph, containing "STRUCTURE_3pmx", 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_3pmx\| PDB=3pmx \| SCENE= }}		{{STRUCTURE_3pmx\| PDB=3pmx \| SCENE= }}

	===Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator===		===Ligand-binding domain of GluA2 (flip) ionotropic glutamate receptor in complex with an allosteric modulator===


	~~<!--~~
	~~The line below this paragraph, {{ABSTRACT_PUBMED_21190850}}, adds the Publication Abstract to the page~~
	~~(as it appears on PubMed at http://www.pubmed.gov), where 21190850 is the PubMed ID number.~~
	~~-->~~
	{{ABSTRACT_PUBMED_21190850}}		{{ABSTRACT_PUBMED_21190850}}

	==About this Structure==		==About this Structure==
	[[3pmx]] is a 1 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=3PMX OCA].		[[3pmx]] is a 1 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=3PMX OCA].

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

	==Reference==		==Reference==
	<ref group="xtra">PMID:~~21190850~~</ref><references group="xtra"/>		<ref group="xtra">PMID:021190850</ref><references group="xtra"/>
	[[Category: Rattus norvegicus]]		[[Category: Rattus norvegicus]]
	[[Category: Brown, C I.]]		[[Category: Brown, C I.]]
Line 39:		Line 31:
	[[Category: Rankovic, Z.]]		[[Category: Rankovic, Z.]]
	[[Category: Smith, L.]]		[[Category: Smith, L.]]
			[[Category: Chimera protein]]
			[[Category: Fusion protein]]
			[[Category: Membrane protein]]
			[[Category: Transport protein]]

OCA at 12:33, 26 January 2011

2011-01-26T12:33:49Z

← Older revision		Revision as of 12:33, 26 January 2011
Line 1:		Line 1:
	[[Image:3pmx.~~jpg~~\|left\|200px]]		[[Image:3pmx.png\|left\|200px]]

	<!--		<!--

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

2011-01-12T05:19:11Z

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

← Older revision	Revision as of 05:19, 12 January 2011
(No difference)