6uzg - Revision history

OCA at 08:01, 11 October 2023

OCA — Wed, 11 Oct 2023 08:01:11 GMT

←Older revision		Revision as of 08:01, 11 October 2023
Line 3:		Line 3:
	<StructureSection load='6uzg' size='340' side='right'caption='[[6uzg]], [[Resolution\|resolution]] 1.94Å' scene=''>		<StructureSection load='6uzg' size='340' side='right'caption='[[6uzg]], [[Resolution\|resolution]] 1.94Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6uzg]] is a 2 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=6UZG OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6UZG FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6uzg]] is a 2 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=6UZG OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6UZG FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat"~~><scene name~~=~~'pdbligand=GLY:GLYCINE'>GLY</scene~~>, ~~<scene name='pdbligand=QM1:3-(carboxymethyl)pyridine-2-carboxylic+acid'>QM1</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]] 1.94Å</td></tr>
-	<tr id='~~gene~~'><td class="sblockLbl"><b>[[~~Gene~~\|~~Gene~~:]]</b></td><td class="sblockDat">~~Grin1, Nmdar1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode~~=~~Info&srchmode~~=~~5&id=10116 Buffalo rat]), Grin2a ([http~~:/~~/www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode~~=~~Info&srchmode~~=~~5&id=10116 Buffalo rat]~~)</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GLY:GLYCINE'>GLY</scene>, <scene name='pdbligand=QM1:3-(carboxymethyl)pyridine-2-carboxylic+acid'>QM1</scene></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=6uzg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6uzg OCA], [~~http~~://pdbe.org/6uzg PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=6uzg RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/6uzg PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=6uzg 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=6uzg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6uzg OCA], [https://pdbe.org/6uzg PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6uzg RCSB], [https://www.ebi.ac.uk/pdbsum/6uzg PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6uzg ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/NMDZ1_RAT NMDZ1_RAT]] NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. Plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. It mediates neuronal functions in glutamate neurotransmission. Is involved in the cell surface targeting of NMDA receptors.<ref>PMID:15996549</ref> [[http://www.uniprot.org/uniprot/NMDE1_RAT NMDE1_RAT]] NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Activation requires binding of agonist to both types of subunits.	+	[https://www.uniprot.org/uniprot/NMDZ1_RAT NMDZ1_RAT] NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. Plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. It mediates neuronal functions in glutamate neurotransmission. Is involved in the cell surface targeting of NMDA receptors.<ref>PMID:15996549</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 19:		Line 19:
	</div>		</div>
	<div class="pdbe-citations 6uzg" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 6uzg" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Glutamate receptor 3D structures\|Glutamate receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: Buffalo rat]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~Furukawa, H~~]]	+	[[Category: Rattus norvegicus]]
-	[[Category: ~~Wang, J X~~]]	+	[[Category: Furukawa H]]
-	[[Category: ~~Agonist]]~~	+	[[Category: Wang JX]]
-	~~[[Category: Ligand-binding domain]]~~	+
-	~~[[Category: Membrane protein]]~~	+
-	~~[[Category: Nmdar~~]]	+

OCA at 09:09, 5 February 2020

OCA — Wed, 05 Feb 2020 09:09:32 GMT

←Older revision		Revision as of 09:09, 5 February 2020
Line 3:		Line 3:
	<StructureSection load='6uzg' size='340' side='right'caption='[[6uzg]], [[Resolution\|resolution]] 1.94Å' scene=''>		<StructureSection load='6uzg' size='340' side='right'caption='[[6uzg]], [[Resolution\|resolution]] 1.94Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6uzg]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6UZG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6UZG FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6uzg]] is a 2 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=6UZG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6UZG FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GLY:GLYCINE'>GLY</scene>, <scene name='pdbligand=QM1:3-(carboxymethyl)pyridine-2-carboxylic+acid'>QM1</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GLY:GLYCINE'>GLY</scene>, <scene name='pdbligand=QM1:3-(carboxymethyl)pyridine-2-carboxylic+acid'>QM1</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Grin1, Nmdar1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat]), Grin2a ([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=6uzg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6uzg OCA], [http://pdbe.org/6uzg PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6uzg RCSB], [http://www.ebi.ac.uk/pdbsum/6uzg PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6uzg ProSAT]</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=6uzg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6uzg OCA], [http://pdbe.org/6uzg PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6uzg RCSB], [http://www.ebi.ac.uk/pdbsum/6uzg PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6uzg ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/NMDZ1_RAT NMDZ1_RAT]] NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. Plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. It mediates neuronal functions in glutamate neurotransmission. Is involved in the cell surface targeting of NMDA receptors.<ref>PMID:15996549</ref> [[http://www.uniprot.org/uniprot/NMDE1_RAT NMDE1_RAT]] NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Activation requires binding of agonist to both types of subunits.		[[http://www.uniprot.org/uniprot/NMDZ1_RAT NMDZ1_RAT]] NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. Plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. It mediates neuronal functions in glutamate neurotransmission. Is involved in the cell surface targeting of NMDA receptors.<ref>PMID:15996549</ref> [[http://www.uniprot.org/uniprot/NMDE1_RAT NMDE1_RAT]] NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Activation requires binding of agonist to both types of subunits.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	N-Methyl-D-aspartate receptors (NMDARs) play critical roles in the central nervous system. Their heterotetrameric composition generates subtypes with distinct functional properties and spatio-temporal distribution in the brain, raising the possibility for subtype-specific targeting by pharmacological means for treatment of neurological diseases. While specific compounds for GluN2A and GluN2B-containing NMDARs are well established, those that target GluN2C and GluN2D are currently underdeveloped with low potency and uncharacterized binding modes. Here, using electrophysiology and X-ray crystallography, we show that UBP791 ((2S,3R)-1-(7-(2-carboxyethyl)phenanthrene-2-carbonyl)piperazine-2,3-dicarboxyl ic acid) inhibits GluN2C/2D with 40-fold selectivity over GluN2A-containing receptors, and that a methionine and a lysine residue in the ligand binding pocket (GluN2D-Met763/Lys766, GluN2C-Met736/Lys739) are the critical molecular elements for the subtype-specific binding. These findings led to development of UBP1700 ((2S,3R)-1-(7-(2-carboxyvinyl)phenanthrene-2-carbonyl)piperazine-2,3-dicarboxyl ic acid) which shows over 50-fold GluN2C/2D-selectivity over GluN2A with potencies in the low nanomolar range. Our study shows that the L-glutamate binding site can be targeted for GluN2C/2D-specific inhibition.
		+
		+	Structural basis of subtype-selective competitive antagonism for GluN2C/2D-containing NMDA receptors.,Wang JX, Irvine MW, Burnell ES, Sapkota K, Thatcher RJ, Li M, Simorowski N, Volianskis A, Collingridge GL, Monaghan DT, Jane DE, Furukawa H Nat Commun. 2020 Jan 22;11(1):423. doi: 10.1038/s41467-020-14321-0. PMID:31969570<ref>PMID:31969570</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 6uzg" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Buffalo rat]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Furukawa, H]]		[[Category: Furukawa, H]]

OCA at 15:45, 29 January 2020

OCA — Wed, 29 Jan 2020 15:45:31 GMT

←Older revision		Revision as of 15:45, 29 January 2020
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 6uzg is ~~ON HOLD until Paper Publication~~	+	==Crystal structure of GLUN1/GLUN2A-4M mutant ligand-binding domain in complex with glycine and homoquinolinic acid==
-		+	<StructureSection load='6uzg' size='340' side='right'caption='[[6uzg]], [[Resolution\|resolution]] 1.94Å' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[6uzg]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6UZG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6UZG FirstGlance]. <br>
-	~~Description~~:	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GLY:GLYCINE'>GLY</scene>, <scene name='pdbligand=QM1:3-(carboxymethyl)pyridine-2-carboxylic+acid'>QM1</scene></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	<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=6uzg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6uzg OCA], [http://pdbe.org/6uzg PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6uzg RCSB], [http://www.ebi.ac.uk/pdbsum/6uzg PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6uzg ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/NMDZ1_RAT NMDZ1_RAT]] NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. Plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. It mediates neuronal functions in glutamate neurotransmission. Is involved in the cell surface targeting of NMDA receptors.<ref>PMID:15996549</ref> [[http://www.uniprot.org/uniprot/NMDE1_RAT NMDE1_RAT]] NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Activation requires binding of agonist to both types of subunits.
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Furukawa, H]]
		+	[[Category: Wang, J X]]
		+	[[Category: Agonist]]
		+	[[Category: Ligand-binding domain]]
		+	[[Category: Membrane protein]]
		+	[[Category: Nmdar]]

OCA at 13:43, 11 December 2019

OCA — Wed, 11 Dec 2019 13:43:14 GMT

←Older revision		Revision as of 13:43, 11 December 2019
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6uzg is ON HOLD	+	The entry 6uzg is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "6uzg" [edit=sysop:move=sysop]

OCA — Wed, 20 Nov 2019 13:59:33 GMT

Protected "6uzg" [edit=sysop:move=sysop]

←Older revision

Revision as of 13:59, 20 November 2019

OCA: New page: '''Unreleased structure''' The entry 6uzg is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 20 Nov 2019 13:59:31 GMT

New page: '''Unreleased structure''' The entry 6uzg is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 6uzg is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]