OCA at 09:21, 19 April 2023

2023-04-19T09:21:57Z

←Older revision		Revision as of 09:21, 19 April 2023
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-	'''Unreleased structure'''

-	~~The entry~~ 7yae is ~~ON HOLD until Paper~~ Publication	+	==Octreotide-bound SSTR2-Gi complex==
		+	<StructureSection load='7yae' size='340' side='right'caption='[[7yae]], [[Resolution\|resolution]] 3.37Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[7yae]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens], [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus] and [https://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7YAE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7YAE FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=DPN:D-PHENYLALANINE'>DPN</scene>, <scene name='pdbligand=DTR:D-TRYPTOPHAN'>DTR</scene>, <scene name='pdbligand=THO:REDUCED+THREONINE'>THO</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=7yae FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7yae OCA], [https://pdbe.org/7yae PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7yae RCSB], [https://www.ebi.ac.uk/pdbsum/7yae PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7yae ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[https://www.uniprot.org/uniprot/GNAI1_HUMAN GNAI1_HUMAN] Guanine nucleotide-binding proteins (G proteins) are involved as modulators or transducers in various transmembrane signaling systems. The G(i) proteins are involved in hormonal regulation of adenylate cyclase: they inhibit the cyclase in response to beta-adrenergic stimuli. The inactive GDP-bound form prevents the association of RGS14 with centrosomes and is required for the translocation of RGS14 from the cytoplasm to the plasma membrane. May play a role in cell division.<ref>PMID:17635935</ref> <ref>PMID:17264214</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Somatostatin receptor 2 (SSTR2) is highly expressed in neuroendocrine tumors and represents as a therapeutic target. Several peptide analogs mimicking the endogenous ligand somatostatin are available for clinical use, but poor therapeutic effects occur in a subset of patients, which may be correlated with subtype selectivity or cell surface expression. Here, we clarify the signal bias profiles of the first-generation peptide drug octreotide and a new-generation small molecule paltusotine by evaluating their pharmacological characteristics. We then perform cryo-electron microscopy analysis of SSTR2-Gi complexes to determine how the drugs activate SSTR2 in a selective manner. In this work, we decipher the mechanism of ligand recognition, subtype selectivity and signal bias property of SSTR2 sensing octreotide and paltusotine, which may aid in designing therapeutic drugs with specific pharmacological profiles against neuroendocrine tumors.

-	~~Authors~~:	+	Prospect of acromegaly therapy: molecular mechanism of clinical drugs octreotide and paltusotine.,Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z Nat Commun. 2023 Feb 21;14(1):962. doi: 10.1038/s41467-023-36673-z. PMID:36810324<ref>PMID:36810324</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased~~ Structures]]	+	</div>
		+	<div class="pdbe-citations 7yae" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Homo sapiens]]
		+	[[Category: Large Structures]]
		+	[[Category: Mus musculus]]
		+	[[Category: Synthetic construct]]
		+	[[Category: Shao Z]]
		+	[[Category: Zhao J]]

OCA at 04:40, 9 November 2022

2022-11-09T04:40:26Z

←Older revision		Revision as of 04:40, 9 November 2022
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	'''Unreleased structure'''		'''Unreleased structure'''

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

	Authors:		Authors:

OCA at 03:45, 26 October 2022

2022-10-26T03:45:23Z

←Older revision		Revision as of 03:45, 26 October 2022
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 7yae is ON HOLD ~~until Paper Publication~~	+	The entry 7yae is ON HOLD

	Authors:		Authors:

OCA at 03:27, 18 August 2022

2022-08-18T03:27:17Z

←Older revision		Revision as of 03:27, 18 August 2022
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	'''Unreleased structure'''		'''Unreleased structure'''

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

	Authors:		Authors:

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

2022-07-06T14:57:47Z

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

←Older revision

Revision as of 14:57, 6 July 2022

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

2022-07-06T14:57:46Z

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

New page