3n7s - Revision history

OCA at 06:14, 26 October 2022

OCA — Wed, 26 Oct 2022 06:14:30 GMT

←Older revision		Revision as of 06:14, 26 October 2022
Line 1:		Line 1:

	==Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism==		==Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism==
-	<StructureSection load='3n7s' size='340' side='right' caption='[[3n7s]], [[Resolution\|resolution]] 2.10Å' scene=''>	+	<StructureSection load='3n7s' size='340' side='right'caption='[[3n7s]], [[Resolution\|resolution]] 2.10Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3n7s]] is a 4 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=3N7S OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3N7S FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3n7s]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3N7S OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3N7S FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3N6:N-{(1S)-5-AMINO-1-[(4-PYRIDIN-4-YLPIPERAZIN-1-YL)CARBONYL]PENTYL}-3,5-DIBROMO-NALPHA-{[4-(2-OXO-1,4-DIHYDROQUINAZOLIN-3(2H)-YL)PIPERIDIN-1-YL]CARBONYL}-D-TYROSINAMIDE'>3N6</scene>, <scene name='pdbligand=3N7:N~4~-(5-CYCLOPROPYL-1H-PYRAZOL-3-YL)-N~2~-1H-INDAZOL-5-YL-6-METHYLPYRIMIDINE-2,4-DIAMINE'>3N7</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=3N6:N-{(1S)-5-AMINO-1-[(4-PYRIDIN-4-YLPIPERAZIN-1-YL)CARBONYL]PENTYL}-3,5-DIBROMO-NALPHA-{[4-(2-OXO-1,4-DIHYDROQUINAZOLIN-3(2H)-YL)PIPERIDIN-1-YL]CARBONYL}-D-TYROSINAMIDE'>3N6</scene>, <scene name='pdbligand=3N7:N~4~-(5-CYCLOPROPYL-1H-PYRAZOL-3-YL)-N~2~-1H-INDAZOL-5-YL-6-METHYLPYRIMIDINE-2,4-DIAMINE'>3N7</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">[[3n7p\|3n7p]], [[3n7r\|3n7r]]</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=3n7s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3n7s OCA], [https://pdbe.org/3n7s PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3n7s RCSB], [https://www.ebi.ac.uk/pdbsum/3n7s PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3n7s ProSAT]</span></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CALCRL, CALRL_HUMAN, CGRPR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN]), RAMP1, RAMP1_HUMAN ([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=3n7s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3n7s OCA], [~~http~~://pdbe.org/3n7s PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3n7s RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3n7s PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=3n7s ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/CALRL_HUMAN CALRL_HUMAN]] Receptor for calcitonin-gene-related peptide (CGRP) together with RAMP1 and receptor for adrenomedullin together with RAMP3 (By similarity). Receptor for adrenomedullin together with RAMP2. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.<ref>PMID:22102369</ref> [[http://www.uniprot.org/uniprot/RAMP1_HUMAN RAMP1_HUMAN]] Transports the calcitonin gene-related peptide type 1 receptor (CALCRL) to the plasma membrane. Acts as a receptor for calcitonin-gene-related peptide (CGRP) together with CALCRL.<ref>PMID:9620797</ref>	+	[https://www.uniprot.org/uniprot/CALRL_HUMAN CALRL_HUMAN] Receptor for calcitonin-gene-related peptide (CGRP) together with RAMP1 and receptor for adrenomedullin together with RAMP3 (By similarity). Receptor for adrenomedullin together with RAMP2. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.<ref>PMID:22102369</ref>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
	Check<jmol>		Check<jmol>
	<jmolCheckbox>		<jmolCheckbox>
-	<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/n7/3n7s_consurf.spt"</scriptWhenChecked>	+	<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/n7/3n7s_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 34:		Line 32:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
-	[[Category: ~~Haar, E Ter~~]]	+	[[Category: Large Structures]]
-	[[Category: ~~Antagonist]]~~	+	[[Category: Ter Haar E]]
-	~~[[Category: Class b gpcr]]~~	+
-	~~[[Category: Gpcr]]~~	+
-	~~[[Category: Membrane protein]]~~	+
-	~~[[Category: Migraine]]~~	+
-	~~[[Category: Olcegepant]]~~	+
-	~~[[Category: Telcagepant~~]]	+

OCA at 12:38, 4 August 2016

OCA — Thu, 04 Aug 2016 12:38:55 GMT

←Older revision		Revision as of 12:38, 4 August 2016
Line 1:		Line 1:
		+
	==Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism==		==Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism==
	<StructureSection load='3n7s' size='340' side='right' caption='[[3n7s]], [[Resolution\|resolution]] 2.10Å' scene=''>		<StructureSection load='3n7s' size='340' side='right' caption='[[3n7s]], [[Resolution\|resolution]] 2.10Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3n7s]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/~~Homo_sapiens Homo sapiens~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3N7S OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3N7S FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3n7s]] is a 4 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=3N7S OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3N7S FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3N6:N-{(1S)-5-AMINO-1-[(4-PYRIDIN-4-YLPIPERAZIN-1-YL)CARBONYL]PENTYL}-3,5-DIBROMO-NALPHA-{[4-(2-OXO-1,4-DIHYDROQUINAZOLIN-3(2H)-YL)PIPERIDIN-1-YL]CARBONYL}-D-TYROSINAMIDE'>3N6</scene>, <scene name='pdbligand=3N7:N~4~-(5-CYCLOPROPYL-1H-PYRAZOL-3-YL)-N~2~-1H-INDAZOL-5-YL-6-METHYLPYRIMIDINE-2,4-DIAMINE'>3N7</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=3N6:N-{(1S)-5-AMINO-1-[(4-PYRIDIN-4-YLPIPERAZIN-1-YL)CARBONYL]PENTYL}-3,5-DIBROMO-NALPHA-{[4-(2-OXO-1,4-DIHYDROQUINAZOLIN-3(2H)-YL)PIPERIDIN-1-YL]CARBONYL}-D-TYROSINAMIDE'>3N6</scene>, <scene name='pdbligand=3N7:N~4~-(5-CYCLOPROPYL-1H-PYRAZOL-3-YL)-N~2~-1H-INDAZOL-5-YL-6-METHYLPYRIMIDINE-2,4-DIAMINE'>3N7</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">[[3n7p\|3n7p]], [[3n7r\|3n7r]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3n7p\|3n7p]], [[3n7r\|3n7r]]</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CALCRL, CALRL_HUMAN, CGRPR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 ~~Homo sapiens~~]), RAMP1, RAMP1_HUMAN ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 ~~Homo sapiens~~])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CALCRL, CALRL_HUMAN, CGRPR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN]), RAMP1, RAMP1_HUMAN ([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=3n7s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3n7s OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3n7s RCSB], [http://www.ebi.ac.uk/pdbsum/3n7s 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=3n7s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3n7s OCA], [http://pdbe.org/3n7s PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3n7s RCSB], [http://www.ebi.ac.uk/pdbsum/3n7s PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3n7s ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[http://www.uniprot.org/uniprot/RAMP1_HUMAN RAMP1_HUMAN]] Transports the calcitonin gene-related peptide type 1 receptor (CALCRL) to the plasma membrane. Acts as a receptor for calcitonin-gene-related peptide (CGRP) together with CALCRL.<ref>PMID:9620797</ref>	+	[[http://www.uniprot.org/uniprot/CALRL_HUMAN CALRL_HUMAN]] Receptor for calcitonin-gene-related peptide (CGRP) together with RAMP1 and receptor for adrenomedullin together with RAMP3 (By similarity). Receptor for adrenomedullin together with RAMP2. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.<ref>PMID:22102369</ref> [[http://www.uniprot.org/uniprot/RAMP1_HUMAN RAMP1_HUMAN]] Transports the calcitonin gene-related peptide type 1 receptor (CALCRL) to the plasma membrane. Acts as a receptor for calcitonin-gene-related peptide (CGRP) together with CALCRL.<ref>PMID:9620797</ref>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
Line 18:		Line 19:
	<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=3n7s ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
Line 28:		Line 29:
	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 3n7s" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Haar, E Ter]]		[[Category: Haar, E Ter]]
	[[Category: Antagonist]]		[[Category: Antagonist]]

OCA at 14:36, 24 December 2014

OCA — Wed, 24 Dec 2014 14:36:37 GMT

←Older revision		Revision as of 14:36, 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=3n7s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3n7s OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3n7s RCSB], [http://www.ebi.ac.uk/pdbsum/3n7s 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=3n7s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3n7s OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3n7s RCSB], [http://www.ebi.ac.uk/pdbsum/3n7s PDBsum]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/RAMP1_HUMAN RAMP1_HUMAN]] Transports the calcitonin gene-related peptide type 1 receptor (CALCRL) to the plasma membrane. Acts as a receptor for calcitonin-gene-related peptide (CGRP) together with CALCRL.<ref>PMID:9620797</ref>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]

OCA at 15:11, 18 December 2014

OCA — Thu, 18 Dec 2014 15:11:01 GMT

←Older revision		Revision as of 15:11, 18 December 2014
Line 1:		Line 1:
-	~~{{STRUCTURE_3n7s\| PDB=3n7s \| SCENE= }}~~	+	==Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism==
-	===Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism===	+	<StructureSection load='3n7s' size='340' side='right' caption='[[3n7s]], [[Resolution\|resolution]] 2.10Å' scene=''>
-	{{~~ABSTRACT_PUBMED_20826335}~~}	+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[3n7s]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3N7S OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3N7S FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3N6:N-{(1S)-5-AMINO-1-[(4-PYRIDIN-4-YLPIPERAZIN-1-YL)CARBONYL]PENTYL}-3,5-DIBROMO-NALPHA-{[4-(2-OXO-1,4-DIHYDROQUINAZOLIN-3(2H)-YL)PIPERIDIN-1-YL]CARBONYL}-D-TYROSINAMIDE'>3N6</scene>, <scene name='pdbligand=3N7:N~4~-(5-CYCLOPROPYL-1H-PYRAZOL-3-YL)-N~2~-1H-INDAZOL-5-YL-6-METHYLPYRIMIDINE-2,4-DIAMINE'>3N7</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">[[3n7p\|3n7p]], [[3n7r\|3n7r]]</td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CALCRL, CALRL_HUMAN, CGRPR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]), RAMP1, RAMP1_HUMAN ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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=3n7s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3n7s OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3n7s RCSB], [http://www.ebi.ac.uk/pdbsum/3n7s 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/n7/3n7s_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 ==
		+	Dysregulation of the calcitonin gene-related peptide (CGRP), a potent vasodilator, is directly implicated in the pathogenesis of migraine. CGRP binds to and signals through the CGRP receptor (CGRP-R), a heterodimer containing the calcitonin receptor-like receptor (CLR), a class B GPCR, and RAMP1, a receptor activity-modifying protein. We have solved the crystal structure of the CLR/RAMP1 N-terminal ectodomain heterodimer, revealing how RAMPs bind to and potentially modulate the activities of the CLR GPCR subfamily. We also report the structures of CLR/RAMP1 in complex with the clinical receptor antagonists olcegepant (BIBN4096BS) and telcagepant (MK0974). Both drugs act by blocking access to the peptide-binding cleft at the interface of CLR and RAMP1. These structures illustrate, for the first time, how small molecules bind to and modulate the activity of a class B GPCR, and highlight the challenges of designing potent receptor antagonists for the treatment of migraine and other class B GPCR-related diseases.

-	~~==Function==~~	+	Crystal structure of the ectodomain complex of the CGRP receptor, a class-B GPCR, reveals the site of drug antagonism.,ter Haar E, Koth CM, Abdul-Manan N, Swenson L, Coll JT, Lippke JA, Lepre CA, Garcia-Guzman M, Moore JM Structure. 2010 Sep 8;18(9):1083-93. PMID:20826335<ref>PMID:20826335</ref>
-	~~[[http://www.uniprot.org/uniprot/RAMP1_HUMAN RAMP1_HUMAN]] Transports~~ the ~~calcitonin gene~~-~~related peptide type 1 receptor (CALCRL) to~~ the ~~plasma membrane~~. ~~Acts as a receptor for calcitonin~~-~~gene~~-~~related peptide~~ (~~CGRP~~) ~~together with CALCRL~~.<ref>PMID:~~9620797~~</ref>	+

-	~~==About this Structure==~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[3n7s]] is~~ a ~~4 chain structure with sequence from [http://en~~.~~wikipedia~~.~~org/wiki/Homo_sapiens Homo sapiens]~~. ~~Full crystallographic information is available from [http:~~/~~/oca.weizmann.ac.il/oca-bin/ocashort?id=3N7S OCA].~~	+	</div>
-		+	== References ==
-	==~~Reference~~==	+	<references/>
-	~~<ref group="xtra">PMID:020826335</ref>~~<references ~~group="xtra"~~/><~~references~~/>	+	__TOC__
		+	</StructureSection>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
-	[[Category: Haar, E Ter.]]	+	[[Category: Haar, E Ter]]
	[[Category: Antagonist]]		[[Category: Antagonist]]
	[[Category: Class b gpcr]]		[[Category: Class b gpcr]]

OCA: Protected "3n7s" [edit=sysop:move=sysop]

OCA — Wed, 17 Apr 2013 21:16:32 GMT

Protected "3n7s" [edit=sysop:move=sysop]

←Older revision

Revision as of 21:16, 17 April 2013

OCA at 21:16, 17 April 2013

OCA — Wed, 17 Apr 2013 21:16:28 GMT

←Older revision		Revision as of 21:16, 17 April 2013
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-	{{Seed}}
-	[[Image:3n7s.png\|left\|200px]]
-
-	<!--
-	The line below this paragraph, containing "STRUCTURE_3n7s", 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_3n7s\| PDB=3n7s \| SCENE= }}		{{STRUCTURE_3n7s\| PDB=3n7s \| SCENE= }}
-
	===Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism===		===Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism===
		+	{{ABSTRACT_PUBMED_20826335}}

-		+	==Function==
-	~~<!--~~	+	[[http://www.uniprot.org/uniprot/RAMP1_HUMAN RAMP1_HUMAN]] Transports the calcitonin gene-related peptide type 1 receptor (CALCRL) to the plasma membrane. Acts as a receptor for calcitonin-gene-related peptide (CGRP) together with CALCRL.<ref>PMID:9620797</ref>
-	~~The line below this paragraph, {{ABSTRACT_PUBMED_20826335}}, adds the Publication Abstract to the page~~	+
-	~~(as it appears on PubMed at~~ http://www.~~pubmed~~.~~gov~~)~~, where 20826335 is~~ the ~~PubMed ID number~~.	+
-	-->	+
-	~~{{ABSTRACT_PUBMED_20826335}}~~	+

	==About this Structure==		==About this Structure==
-	~~3N7S~~ is a 4 ~~chains~~ structure with ~~sequences~~ from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3N7S OCA].	+	[[3n7s]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3N7S OCA].

	==Reference==		==Reference==
-	<ref group="xtra">PMID:~~20826335~~</ref><references group="xtra"/>	+	<ref group="xtra">PMID:020826335</ref><references group="xtra"/><references/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Haar, E Ter.]]		[[Category: Haar, E Ter.]]
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	[[Category: Olcegepant]]		[[Category: Olcegepant]]
	[[Category: Telcagepant]]		[[Category: Telcagepant]]
-
-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Sep 22 14:23:42 2010''

OCA at 11:14, 22 September 2010

OCA — Wed, 22 Sep 2010 11:14:44 GMT

←Older revision		Revision as of 11:14, 22 September 2010
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	{{Seed}}		{{Seed}}
-	[[Image:3n7s.~~jpg~~\|left\|200px]]	+	[[Image:3n7s.png\|left\|200px]]

	<!--		<!--
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	===Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism===		===Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism===

		+
		+	<!--
		+	The line below this paragraph, {{ABSTRACT_PUBMED_20826335}}, adds the Publication Abstract to the page
		+	(as it appears on PubMed at http://www.pubmed.gov), where 20826335 is the PubMed ID number.
		+	-->
		+	{{ABSTRACT_PUBMED_20826335}}

	==About this Structure==		==About this Structure==
	3N7S is a 4 chains structure with sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3N7S OCA].		3N7S is a 4 chains structure with sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3N7S OCA].
		+
		+	==Reference==
		+	<ref group="xtra">PMID:20826335</ref><references group="xtra"/>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Haar, E Ter.]]		[[Category: Haar, E Ter.]]
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	[[Category: Telcagepant]]		[[Category: Telcagepant]]

-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Sep ~~15 10~~:50:51 2010''	+	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Sep 22 14:23:42 2010''

OCA at 07:42, 15 September 2010

OCA — Wed, 15 Sep 2010 07:42:11 GMT

←Older revision		Revision as of 07:42, 15 September 2010
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-	~~'''Unreleased structure'''~~	+	{{Seed}}
		+	[[Image:3n7s.jpg\|left\|200px]]

-	The ~~entry 3n7s~~ is ~~ON HOLD~~ ~~until Paper Publication~~	+	<!--
		+	The line below this paragraph, containing "STRUCTURE_3n7s", 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_3n7s\| PDB=3n7s \| SCENE= }}

-	~~Authors: Ter Haar~~, E.	+	===Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism===

-	Description: Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism

-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed ~~Jun 16 08~~:29:24 2010''	+	==About this Structure==
		+	3N7S is a 4 chains structure with sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3N7S OCA].
		+	[[Category: Homo sapiens]]
		+	[[Category: Haar, E Ter.]]
		+	[[Category: Antagonist]]
		+	[[Category: Class b gpcr]]
		+	[[Category: Gpcr]]
		+	[[Category: Membrane protein]]
		+	[[Category: Migraine]]
		+	[[Category: Olcegepant]]
		+	[[Category: Telcagepant]]
		+
		+	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Sep 15 10:50:51 2010''

OCA at 04:24, 16 June 2010

OCA — Wed, 16 Jun 2010 04:24:23 GMT

←Older revision		Revision as of 04:24, 16 June 2010
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 3n7s is ON HOLD	+	The entry 3n7s is ON HOLD until Paper Publication

	Authors: Ter Haar, E.		Authors: Ter Haar, E.
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	Description: Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism		Description: Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism

-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Thu~~ Jun ~~10 10~~:58:25 2010''	+	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jun 16 08:29:24 2010''

OCA at 06:53, 10 June 2010

OCA — Thu, 10 Jun 2010 06:53:38 GMT

←Older revision		Revision as of 06:53, 10 June 2010
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	The entry 3n7s is ON HOLD		The entry 3n7s is ON HOLD

-	Authors: Ter Haar, E~~., Koth, C.M., Abdul-Manan, N., Swenson, L., Coll, J.T., Lippke, J.A., Lepre, C.A., Garcia-Guzman, M., Moore, J.M~~.	+	Authors: Ter Haar, E.

	Description: Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism		Description: Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism

-	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Wed~~ Jun ~~2 08~~:29:51 2010''	+	''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Jun 10 10:58:25 2010''