6luq - Revision history

OCA at 14:54, 29 November 2023

OCA — Wed, 29 Nov 2023 14:54:32 GMT

←Older revision		Revision as of 14:54, 29 November 2023
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	<StructureSection load='6luq' size='340' side='right'caption='[[6luq]], [[Resolution\|resolution]] 3.10Å' scene=''>		<StructureSection load='6luq' size='340' side='right'caption='[[6luq]], [[Resolution\|resolution]] 3.10Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6luq]] is a 1 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6LUQ OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6LUQ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6luq]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_virus_T4 Escherichia virus T4] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6LUQ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6LUQ FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat">~~<scene name='pdbligand=GMJ:4~~-[~~4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl~~]-1~~-(4-fluorophenyl)butan-1-one'>GMJ</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</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]] 3.1Å</td></tr>
-	<tr id='~~gene~~'><td class="sblockLbl"><b>[[~~Gene~~\|~~Gene~~:]]</b></td><td class="sblockDat"~~>DRD2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&~~id=~~9606 HUMAN])</td~~><~~/tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GMJ:4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one'>GMJ</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene></td></tr>
-	~~<tr id~~='~~activity'><td class~~=~~"sblockLbl"><b>Activity~~:~~</b~~></td><~~td class~~=~~"sblockDat"><span class~~=~~'plainlinks~~'>~~[http://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17]~~ </~~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=6luq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6luq OCA], [https://pdbe.org/6luq PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6luq RCSB], [https://www.ebi.ac.uk/pdbsum/6luq PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6luq 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=6luq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6luq OCA], [~~http~~://pdbe.org/6luq PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=6luq RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/6luq PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=6luq ProSAT]</span></td></tr>	+
	</table>		</table>
	== Disease ==		== Disease ==
-	[~~[http~~://www.uniprot.org/uniprot/DRD2_HUMAN DRD2_HUMAN]] Myoclonic dystonia 11. The gene represented in this entry may be involved in disease pathogenesis. DRD2 mutations in myoclonic dystonia patients are rare, and their contribution to disease phenotype is unclear (PubMed:10716258).	+	[https://www.uniprot.org/uniprot/DRD2_HUMAN DRD2_HUMAN] Myoclonic dystonia 11. The gene represented in this entry may be involved in disease pathogenesis. DRD2 mutations in myoclonic dystonia patients are rare, and their contribution to disease phenotype is unclear (PubMed:10716258).
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/DRD2_HUMAN DRD2_HUMAN]] Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (By similarity).<ref>PMID:21645528</ref> <ref>PMID:17264214</ref>	+	[https://www.uniprot.org/uniprot/D9IEF7_BPT4 D9IEF7_BPT4] [https://www.uniprot.org/uniprot/DRD2_HUMAN DRD2_HUMAN] Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (By similarity).<ref>PMID:21645528</ref> <ref>PMID:17264214</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	</div>		</div>
	<div class="pdbe-citations 6luq" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 6luq" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Dopamine receptor 3D structures\|Dopamine receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Escherichia virus T4]]
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	~~[[Category: Lysozyme]]~~	+	[[Category: Chen Z]]
-	[[Category: Chen, Z]]	+	[[Category: Cheng J]]
-	[[Category: Cheng, J]]	+	[[Category: Fan L]]
-	[[Category: Fan, L]]	+	[[Category: Luo Z]]
-	[[Category: Luo, Z]]	+	[[Category: Nie F]]
-	[[Category: Nie, F]]	+	[[Category: Qi J]]
-	[[Category: Qi, J]]	+	[[Category: Tan L]]
-	[[Category: Tan, L]]	+	[[Category: Wang S]]
-	[[Category: Wang, S]]	+
-	~~[[Category: D2 dopamine receptor]]~~	+
-	~~[[Category: Dopamine receptor]]~~	+
-	~~[[Category: Gpcr]]~~	+
-	~~[[Category: Haloperidol]]~~	+
-	~~[[Category: Membrane protein~~]]	+

OCA at 07:54, 11 March 2020

OCA — Wed, 11 Mar 2020 07:54:20 GMT

←Older revision		Revision as of 07:54, 11 March 2020
Line 3:		Line 3:
	<StructureSection load='6luq' size='340' side='right'caption='[[6luq]], [[Resolution\|resolution]] 3.10Å' scene=''>		<StructureSection load='6luq' size='340' side='right'caption='[[6luq]], [[Resolution\|resolution]] 3.10Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6luq]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6LUQ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6LUQ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6luq]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6LUQ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6LUQ FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GMJ:4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one'>GMJ</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GMJ:4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one'>GMJ</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">DRD2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </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=6luq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6luq OCA], [http://pdbe.org/6luq PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6luq RCSB], [http://www.ebi.ac.uk/pdbsum/6luq PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6luq 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=6luq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6luq OCA], [http://pdbe.org/6luq PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6luq RCSB], [http://www.ebi.ac.uk/pdbsum/6luq PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6luq ProSAT]</span></td></tr>
Line 12:		Line 13:
	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/DRD2_HUMAN DRD2_HUMAN]] Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (By similarity).<ref>PMID:21645528</ref> <ref>PMID:17264214</ref>		[[http://www.uniprot.org/uniprot/DRD2_HUMAN DRD2_HUMAN]] Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (By similarity).<ref>PMID:21645528</ref> <ref>PMID:17264214</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The D2 dopamine receptor (DRD2) is one of the most well-established therapeutic targets for neuropsychiatric and endocrine disorders. Most clinically approved and investigational drugs that target this receptor are known to be subfamily-selective for all three D2-like receptors, rather than subtype-selective for only DRD2. Here, we report the crystal structure of DRD2 bound to the most commonly used antipsychotic drug, haloperidol. The structures suggest an extended binding pocket for DRD2 that distinguishes it from other D2-like subtypes. A detailed analysis of the structures illuminates key structural determinants essential for DRD2 activation and subtype selectivity. A structure-based and mechanism-driven screening combined with a lead optimization approach yield DRD2 highly selective agonists, which could be used as chemical probes for studying the physiological and pathological functions of DRD2 as well as promising therapeutic leads devoid of promiscuity.
		+
		+	Haloperidol bound D2 dopamine receptor structure inspired the discovery of subtype selective ligands.,Fan L, Tan L, Chen Z, Qi J, Nie F, Luo Z, Cheng J, Wang S Nat Commun. 2020 Feb 26;11(1):1074. doi: 10.1038/s41467-020-14884-y. PMID:32103023<ref>PMID:32103023</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 6luq" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Lysozyme]]		[[Category: Lysozyme]]

OCA at 06:42, 4 March 2020

OCA — Wed, 04 Mar 2020 06:42:26 GMT

←Older revision		Revision as of 06:42, 4 March 2020
Line 1:		Line 1:
-	'''Unreleased structure'''

-	The entry ~~6luq~~ is ~~ON HOLD~~ ~~until Paper Publication~~	+	==Haloperidol bound D2 dopamine receptor structure inspired discovery of subtype selective ligands==
-		+	<StructureSection load='6luq' size='340' side='right'caption='[[6luq]], [[Resolution\|resolution]] 3.10Å' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[6luq]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6LUQ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6LUQ FirstGlance]. <br>
-	~~Description~~:	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GMJ:4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one'>GMJ</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene></td></tr>
-	[[Category: ~~Unreleased Structures~~]]	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </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=6luq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6luq OCA], [http://pdbe.org/6luq PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6luq RCSB], [http://www.ebi.ac.uk/pdbsum/6luq PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6luq ProSAT]</span></td></tr>
		+	</table>
		+	== Disease ==
		+	[[http://www.uniprot.org/uniprot/DRD2_HUMAN DRD2_HUMAN]] Myoclonic dystonia 11. The gene represented in this entry may be involved in disease pathogenesis. DRD2 mutations in myoclonic dystonia patients are rare, and their contribution to disease phenotype is unclear (PubMed:10716258).
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/DRD2_HUMAN DRD2_HUMAN]] Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase (By similarity).<ref>PMID:21645528</ref> <ref>PMID:17264214</ref>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Lysozyme]]
		+	[[Category: Chen, Z]]
		+	[[Category: Cheng, J]]
		+	[[Category: Fan, L]]
		+	[[Category: Luo, Z]]
		+	[[Category: Nie, F]]
		+	[[Category: Qi, J]]
		+	[[Category: Tan, L]]
		+	[[Category: Wang, S]]
		+	[[Category: D2 dopamine receptor]]
		+	[[Category: Dopamine receptor]]
		+	[[Category: Gpcr]]
		+	[[Category: Haloperidol]]
		+	[[Category: Membrane protein]]

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

OCA — Wed, 05 Feb 2020 06:07:24 GMT

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

←Older revision

Revision as of 06:07, 5 February 2020

OCA: New page: '''Unreleased structure''' The entry 6luq is ON HOLD until Paper Publication Authors: Description: Category: Unreleased Structures

OCA — Wed, 05 Feb 2020 06:07:22 GMT

New page: '''Unreleased structure''' The entry 6luq is ON HOLD until Paper Publication Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 6luq is ON HOLD until Paper Publication

Authors:

Description:
[[Category: Unreleased Structures]]