OCA at 06:53, 29 March 2023

OCA — Wed, 29 Mar 2023 06:53:50 GMT

←Older revision		Revision as of 06:53, 29 March 2023
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 8fmz is ~~ON HOLD until Paper~~ Publication	+	==Neurotensin receptor allosterism revealed in complex with a biased allosteric modulator==
		+	<StructureSection load='8fmz' size='340' side='right'caption='[[8fmz]], [[Resolution\|resolution]] 2.59Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[8fmz]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli], [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens], [https://en.wikipedia.org/wiki/Lama_glama Lama glama] and [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8FMZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8FMZ 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=8fmz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8fmz OCA], [https://pdbe.org/8fmz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8fmz RCSB], [https://www.ebi.ac.uk/pdbsum/8fmz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8fmz ProSAT]</span></td></tr>
		+	</table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The NTSR1 neurotensin receptor (NTSR1) is a G protein-coupled receptor (GPCR) found in the brain and peripheral tissues with neurotensin (NTS) being its endogenous peptide ligand. In the brain, NTS modulates dopamine neuronal activity, induces opioid-independent analgesia, and regulates food intake. Recent studies indicate that biasing NTSR1 toward beta-arrestin signaling can attenuate the actions of psychostimulants and other drugs of abuse. Here, we provide the cryoEM structures of NTSR1 ternary complexes with heterotrimeric Gq and GoA with and without the brain-penetrant small-molecule SBI-553. In functional studies, we discovered that SBI-553 displays complex allosteric actions exemplified by negative allosteric modulation for G proteins that are Galpha subunit selective and positive allosteric modulation and agonism for beta-arrestin translocation at NTSR1. Detailed structural analysis of the allosteric binding site illuminated the structural determinants for biased allosteric modulation of SBI-553 on NTSR1.

-	~~Authors~~:	+	Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator.,Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL Biochemistry. 2023 Mar 14. doi: 10.1021/acs.biochem.3c00029. PMID:36917754<ref>PMID:36917754</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased~~ Structures]]	+	</div>
		+	<div class="pdbe-citations 8fmz" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Escherichia coli]]
		+	[[Category: Homo sapiens]]
		+	[[Category: Lama glama]]
		+	[[Category: Large Structures]]
		+	[[Category: Rattus norvegicus]]
		+	[[Category: Diberto JF]]
		+	[[Category: Fay JF]]
		+	[[Category: Kang H]]
		+	[[Category: Krumm BE]]
		+	[[Category: Olsen RHJ]]
		+	[[Category: Roth BL]]
		+	[[Category: Slocum ST]]
		+	[[Category: Strachan RT]]
		+	[[Category: Zhang S]]

OCA at 04:24, 2 March 2023

OCA — Thu, 02 Mar 2023 04:24:21 GMT

←Older revision		Revision as of 04:24, 2 March 2023
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 8fmz is ON HOLD	+	The entry 8fmz is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "8fmz" [edit=sysop:move=sysop]

OCA — Wed, 11 Jan 2023 05:53:23 GMT

Protected "8fmz" [edit=sysop:move=sysop]

←Older revision

Revision as of 05:53, 11 January 2023

OCA: New page: '''Unreleased structure''' The entry 8fmz is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 11 Jan 2023 05:53:23 GMT

New page: '''Unreleased structure''' The entry 8fmz is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 8fmz is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]

8fmz - Revision history

OCA at 06:53, 29 March 2023

OCA at 04:24, 2 March 2023

OCA: Protected "8fmz" [edit=sysop:move=sysop]

OCA: New page: '''Unreleased structure''' The entry 8fmz is ON HOLD Authors: Description: Category: Unreleased Structures