7f83 - Revision history

OCA at 17:11, 29 November 2023

OCA — Wed, 29 Nov 2023 17:11:02 GMT

←Older revision		Revision as of 17:11, 29 November 2023
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	<StructureSection load='7f83' size='340' side='right'caption='[[7f83]], [[Resolution\|resolution]] 2.94Å' scene=''>		<StructureSection load='7f83' size='340' side='right'caption='[[7f83]], [[Resolution\|resolution]] 2.94Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[7f83]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7F83 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7F83 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[7f83]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] 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=7F83 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7F83 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1KQ:2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-[2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonan-7-yl]ethanone'>1KQ</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</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]] 2.94Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1KQ:2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-[2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonan-7-yl]ethanone'>1KQ</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene></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=7f83 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7f83 OCA], [https://pdbe.org/7f83 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7f83 RCSB], [https://www.ebi.ac.uk/pdbsum/7f83 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7f83 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=7f83 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7f83 OCA], [https://pdbe.org/7f83 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7f83 RCSB], [https://www.ebi.ac.uk/pdbsum/7f83 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7f83 ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
-	[[https://www.uniprot.org/uniprot/GHSR_HUMAN GHSR_HUMAN]] Short stature due to GHSR deficiency. The disease is caused by variants affecting the gene represented in this entry.	+	[https://www.uniprot.org/uniprot/GHSR_HUMAN GHSR_HUMAN] Short stature due to GHSR deficiency. The disease is caused by variants affecting the gene represented in this entry.
	== Function ==		== Function ==
-	[[https://www.uniprot.org/uniprot/GHSR_HUMAN GHSR_HUMAN]] Receptor for ghrelin, coupled to G-alpha-11 proteins. Stimulates growth hormone secretion. Binds also other growth hormone releasing peptides (GHRP) (e.g. Met-enkephalin and GHRP-6) as well as non-peptide, low molecular weight secretagogues (e.g. L-692,429, MK-0677, adenosine).<ref>PMID:10604470</ref> <ref>PMID:11322507</ref>	+	[https://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX] Electron-transport protein of unknown function.[https://www.uniprot.org/uniprot/GHSR_HUMAN GHSR_HUMAN] Receptor for ghrelin, coupled to G-alpha-11 proteins. Stimulates growth hormone secretion. Binds also other growth hormone releasing peptides (GHRP) (e.g. Met-enkephalin and GHRP-6) as well as non-peptide, low molecular weight secretagogues (e.g. L-692,429, MK-0677, adenosine).<ref>PMID:10604470</ref> <ref>PMID:11322507</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 24:		Line 25:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Escherichia coli]]
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Shao, Z]]	+	[[Category: Shao Z]]
-	[[Category: Xu, Z]]	+	[[Category: Xu Z]]
-	~~[[Category: Ghrelin]]~~	+
-	~~[[Category: Gpcr]]~~	+
-	~~[[Category: Inverse agonist]]~~	+
-	~~[[Category: Signaling protein~~]]	+

OCA at 07:08, 27 January 2022

OCA — Thu, 27 Jan 2022 07:08:42 GMT

←Older revision		Revision as of 07:08, 27 January 2022
Line 1:		Line 1:

	==Crystal Structure of a receptor in Complex with inverse agonist==		==Crystal Structure of a receptor in Complex with inverse agonist==
-	<StructureSection load='7f83' size='340' side='right'caption='[[7f83]]' scene=''>	+	<StructureSection load='7f83' size='340' side='right'caption='[[7f83]], [[Resolution\|resolution]] 2.94Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7F83 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7F83 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[7f83]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7F83 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7F83 FirstGlance]. <br>
-	</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=7f83 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7f83 OCA], [https://pdbe.org/7f83 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7f83 RCSB], [https://www.ebi.ac.uk/pdbsum/7f83 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7f83 ProSAT]</span></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1KQ:2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-[2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonan-7-yl]ethanone'>1KQ</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene></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=7f83 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7f83 OCA], [https://pdbe.org/7f83 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7f83 RCSB], [https://www.ebi.ac.uk/pdbsum/7f83 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7f83 ProSAT]</span></td></tr>
	</table>		</table>
		+	== Disease ==
		+	[[https://www.uniprot.org/uniprot/GHSR_HUMAN GHSR_HUMAN]] Short stature due to GHSR deficiency. The disease is caused by variants affecting the gene represented in this entry.
		+	== Function ==
		+	[[https://www.uniprot.org/uniprot/GHSR_HUMAN GHSR_HUMAN]] Receptor for ghrelin, coupled to G-alpha-11 proteins. Stimulates growth hormone secretion. Binds also other growth hormone releasing peptides (GHRP) (e.g. Met-enkephalin and GHRP-6) as well as non-peptide, low molecular weight secretagogues (e.g. L-692,429, MK-0677, adenosine).<ref>PMID:10604470</ref> <ref>PMID:11322507</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Much effort has been invested in the investigation of the structural basis of G protein-coupled receptors (GPCRs) activation. Inverse agonists, which can inhibit GPCRs with constitutive activity, are considered useful therapeutic agents, but the molecular mechanism of such ligands remains insufficiently understood. Here, we report a crystal structure of the ghrelin receptor bound to the inverse agonist PF-05190457 and a cryo-electron microscopy structure of the active ghrelin receptor-Go complex bound to the endogenous agonist ghrelin. Our structures reveal a distinct binding mode of the inverse agonist PF-05190457 in the ghrelin receptor, different from the binding mode of agonists and neutral antagonists. Combining the structural comparisons and cellular function assays, we find that a polar network and a notable hydrophobic cluster are required for receptor activation and constitutive activity. Together, our study provides insights into the detailed mechanism of ghrelin receptor binding to agonists and inverse agonists, and paves the way to design specific ligands targeting ghrelin receptors.
		+
		+	Molecular mechanism of agonism and inverse agonism in ghrelin receptor.,Qin J, Cai Y, Xu Z, Ming Q, Ji SY, Wu C, Zhang H, Mao C, Shen DD, Hirata K, Ma Y, Yan W, Zhang Y, Shao Z Nat Commun. 2022 Jan 13;13(1):300. doi: 10.1038/s41467-022-27975-9. PMID:35027551<ref>PMID:35027551</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 7f83" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Shao Z]]	+	[[Category: Shao, Z]]
-	[[Category: Xu Z]]	+	[[Category: Xu, Z]]
		+	[[Category: Ghrelin]]
		+	[[Category: Gpcr]]
		+	[[Category: Inverse agonist]]
		+	[[Category: Signaling protein]]

OCA at 07:27, 19 January 2022

OCA — Wed, 19 Jan 2022 07:27:41 GMT

←Older revision		Revision as of 07:27, 19 January 2022
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 7f83 ~~is ON HOLD until Paper Publication~~	+	==Crystal Structure of a receptor in Complex with inverse agonist==
-		+	<StructureSection load='7f83' size='340' side='right'caption='[[7f83]]' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7F83 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7F83 FirstGlance]. <br>
-	~~Description~~:	+	</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=7f83 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7f83 OCA], [https://pdbe.org/7f83 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7f83 RCSB], [https://www.ebi.ac.uk/pdbsum/7f83 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7f83 ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	</table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Shao Z]]
		+	[[Category: Xu Z]]

OCA at 11:40, 29 December 2021

OCA — Wed, 29 Dec 2021 11:40:11 GMT

←Older revision		Revision as of 11:40, 29 December 2021
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 7f83 is ON HOLD	+	The entry 7f83 is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "7f83" [edit=sysop:move=sysop]

OCA — Wed, 07 Jul 2021 08:42:33 GMT

Protected "7f83" [edit=sysop:move=sysop]

←Older revision

Revision as of 08:42, 7 July 2021

OCA: New page: '''Unreleased structure''' The entry 7f83 is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 07 Jul 2021 08:42:32 GMT

New page: '''Unreleased structure''' The entry 7f83 is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 7f83 is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]