5u09 - Revision history

OCA at 13:17, 4 October 2023

2023-10-04T13:17:24Z

←Older revision		Revision as of 13:17, 4 October 2023
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	==High-resolution crystal structure of the human CB1 cannabinoid receptor==		==High-resolution crystal structure of the human CB1 cannabinoid receptor==
-	<StructureSection load='5u09' size='340' side='right' caption='[[5u09]], [[Resolution\|resolution]] 2.60Å' scene=''>	+	<StructureSection load='5u09' size='340' side='right'caption='[[5u09]], [[Resolution\|resolution]] 2.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5u09]] is a 1 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Human Human~~]. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=5tjv 5tjv]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5U09 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5U09 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5u09]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Pyrococcus_abyssi_GE5 Pyrococcus abyssi GE5]. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=5tjv 5tjv]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5U09 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5U09 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7DY:N-[(2S,3S)-4-(4-CHLOROPHENYL)-3-(3-CYANOPHENYL)BUTAN-2-YL]-2-METHYL-2-{[5-(TRIFLUOROMETHYL)PYRIDIN-2-YL]OXY}PROPANAMIDE'>7DY</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</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]] 2.6Å</td></tr>
-	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CNR1, CNR ([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=7DY:N-[(2S,3S)-4-(4-CHLOROPHENYL)-3-(3-CYANOPHENYL)BUTAN-2-YL]-2-METHYL-2-{[5-(TRIFLUOROMETHYL)PYRIDIN-2-YL]OXY}PROPANAMIDE'>7DY</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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=5u09 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5u09 OCA], [~~http~~://pdbe.org/5u09 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5u09 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5u09 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5u09 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=5u09 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5u09 OCA], [https://pdbe.org/5u09 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5u09 RCSB], [https://www.ebi.ac.uk/pdbsum/5u09 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5u09 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/CNR1_HUMAN CNR1_HUMAN]] Involved in cannabinoid-induced CNS effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide. Inhibits L-type Ca(2+) channel current. Isoform 2 and isoform 3 have altered ligand binding.<ref>PMID:15620723</ref>	+	[https://www.uniprot.org/uniprot/Q9V2J8_PYRAB Q9V2J8_PYRAB] [https://www.uniprot.org/uniprot/CNR1_HUMAN CNR1_HUMAN] Involved in cannabinoid-induced CNS effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide. Inhibits L-type Ca(2+) channel current. Isoform 2 and isoform 3 have altered ligand binding.<ref>PMID:15620723</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 23:		Line 23:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
-	[[Category: ~~Rosenbaum, D~~]]	+	[[Category: Large Structures]]
-	[[Category: ~~Shao, Z H~~]]	+	[[Category: Pyrococcus abyssi GE5]]
-	[[Category: ~~Yin, J~~]]	+	[[Category: Rosenbaum D]]
-	[[Category: ~~Helix~~]]	+	[[Category: Shao ZH]]
-	[[Category: ~~Membrane protein~~]]	+	[[Category: Yin J]]

OCA at 10:19, 22 November 2017

2017-11-22T10:19:49Z

←Older revision		Revision as of 10:19, 22 November 2017
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	<StructureSection load='5u09' size='340' side='right' caption='[[5u09]], [[Resolution\|resolution]] 2.60Å' scene=''>		<StructureSection load='5u09' size='340' side='right' caption='[[5u09]], [[Resolution\|resolution]] 2.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5u09]] is a 1 chain structure. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=5tjv 5tjv]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5U09 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5U09 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5u09]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=5tjv 5tjv]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5U09 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5U09 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7DY:N-[(2S,3S)-4-(4-CHLOROPHENYL)-3-(3-CYANOPHENYL)BUTAN-2-YL]-2-METHYL-2-{[5-(TRIFLUOROMETHYL)PYRIDIN-2-YL]OXY}PROPANAMIDE'>7DY</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</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=7DY:N-[(2S,3S)-4-(4-CHLOROPHENYL)-3-(3-CYANOPHENYL)BUTAN-2-YL]-2-METHYL-2-{[5-(TRIFLUOROMETHYL)PYRIDIN-2-YL]OXY}PROPANAMIDE'>7DY</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</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">CNR1, CNR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=5u09 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5u09 OCA], [http://pdbe.org/5u09 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5u09 RCSB], [http://www.ebi.ac.uk/pdbsum/5u09 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5u09 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=5u09 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5u09 OCA], [http://pdbe.org/5u09 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5u09 RCSB], [http://www.ebi.ac.uk/pdbsum/5u09 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5u09 ProSAT]</span></td></tr>
	</table>		</table>
Line 22:		Line 23:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Rosenbaum, D]]		[[Category: Rosenbaum, D]]
	[[Category: Shao, Z H]]		[[Category: Shao, Z H]]

OCA: Protected "5u09" [edit=sysop:move=sysop]

2016-12-09T19:26:42Z

Protected "5u09" [edit=sysop:move=sysop]

←Older revision

Revision as of 19:26, 9 December 2016

OCA: New page: ==High-resolution crystal structure of the human CB1 cannabinoid receptor==
2016-12-09T19:26:39Z

New page: ==High-resolution crystal structure of the human CB1 cannabinoid receptor== <StructureSection load='5u09' size='340' side='right' caption='5u09, resolution 2.60Å'...

New page

==High-resolution crystal structure of the human CB1 cannabinoid receptor==
<StructureSection load='5u09' size='340' side='right' caption='[[5u09]], [[Resolution|resolution]] 2.60Å' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[5u09]] is a 1 chain structure. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=5tjv 5tjv]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5U09 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5U09 FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7DY:N-[(2S,3S)-4-(4-CHLOROPHENYL)-3-(3-CYANOPHENYL)BUTAN-2-YL]-2-METHYL-2-{[5-(TRIFLUOROMETHYL)PYRIDIN-2-YL]OXY}PROPANAMIDE'>7DY</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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=5u09 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5u09 OCA], [http://pdbe.org/5u09 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5u09 RCSB], [http://www.ebi.ac.uk/pdbsum/5u09 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5u09 ProSAT]</span></td></tr>
</table>
== Function ==
[[http://www.uniprot.org/uniprot/CNR1_HUMAN CNR1_HUMAN]] Involved in cannabinoid-induced CNS effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide. Inhibits L-type Ca(2+) channel current. Isoform 2 and isoform 3 have altered ligand binding.<ref>PMID:15620723</ref>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
The human cannabinoid G-protein-coupled receptors (GPCRs) CB1 and CB2 mediate the functional responses to the endocannabinoids anandamide and 2-arachidonyl glycerol (2-AG), as well as the widely consumed plant (phyto)cannabinoid Delta9-tetrahydrocannabinol (THC)1. The cannabinoid receptors have been the targets of intensive drug discovery efforts owing to the therapeutic potential of modulators for controlling pain2, epilepsy3, obesity4, and other maladies. Although much progress has recently been made in understanding the biophysical properties of GPCRs, investigations of the molecular mechanisms of the cannabinoids and their receptors have lacked high-resolution structural data. We used GPCR engineering and lipidic cubic phase (LCP) crystallization to determine the structure of the human CB1 receptor bound to the inhibitor taranabant at 2.6 A resolution. The extracellular surface of CB1, including the highly conserved membrane-proximal amino-terminal (N-terminal) region, is distinct from other lipid-activated GPCRs and forms a critical part of the ligand binding pocket. Docking studies further demonstrate how this same pocket may accommodate the cannabinoid agonist THC. Our CB1 structure provides an atomic framework for studying cannabinoid receptor function, and will aid the design and optimization of cannabinoid system modulators for therapeutic ends.

High-resolution crystal structure of the human CB1 cannabinoid receptor.,Shao Z, Yin J, Chapman K, Grzemska M, Clark L, Wang J, Rosenbaum DM Nature. 2016 Nov 16. doi: 10.1038/nature20613. PMID:27851727<ref>PMID:27851727</ref>

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 5u09" style="background-color:#fffaf0;"></div>
== References ==
<references/>
TOC
</StructureSection>
[[Category: Rosenbaum, D]]
[[Category: Shao, Z H]]
[[Category: Yin, J]]
[[Category: Helix]]
[[Category: Membrane protein]]