8ea0 - Revision history

OCA at 12:04, 23 October 2024

2024-10-23T12:04:34Z

← Older revision		Revision as of 12:04, 23 October 2024
Line 4:		Line 4:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[8ea0]] is a 1 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=8EA0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8EA0 FirstGlance]. <br>		<table><tr><td colspan='2'>[[8ea0]] is a 1 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=8EA0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8EA0 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=IXO:4-(4,5-DIHYDRO-1,2-OXAZOL-3-YLOXY)-N,N,N-TRIMETHYLBUT-2-YN-1-AMINIUM'>IXO</scene>, <scene name='pdbligand=Y01:CHOLESTEROL+HEMISUCCINATE'>Y01</scene></td></tr>		</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution\|Resolution]] 2.56Å</td></tr>
			<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=IXO:4-(4,5-DIHYDRO-1,2-OXAZOL-3-YLOXY)-N,N,N-TRIMETHYLBUT-2-YN-1-AMINIUM'>IXO</scene>, <scene name='pdbligand=Y01:CHOLESTEROL+HEMISUCCINATE'>Y01</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=8ea0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8ea0 OCA], [https://pdbe.org/8ea0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8ea0 RCSB], [https://www.ebi.ac.uk/pdbsum/8ea0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8ea0 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=8ea0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8ea0 OCA], [https://pdbe.org/8ea0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8ea0 RCSB], [https://www.ebi.ac.uk/pdbsum/8ea0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8ea0 ProSAT]</span></td></tr>
	</table>		</table>
Line 11:		Line 12:
	== Function ==		== Function ==
	[https://www.uniprot.org/uniprot/ACM3_HUMAN ACM3_HUMAN] The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.		[https://www.uniprot.org/uniprot/ACM3_HUMAN ACM3_HUMAN] The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			Designer receptors exclusively activated by designer drugs (DREADDs) represent a powerful chemogenetic technology for the remote control of neuronal activity and cellular signalling(1-4). The muscarinic receptor-based DREADDs are the most widely used chemogenetic tools in neuroscience research. The G(q)-coupled DREADD (hM3Dq) is used to enhance neuronal activity, whereas the G(i/o)-coupled DREADD (hM4Di) is utilized to inhibit neuronal activity(5). Here we report four DREADD-related cryogenic electron microscopy high-resolution structures: a hM3Dq-miniG(q) complex and a hM4Di-miniG(o) complex bound to deschloroclozapine; a hM3Dq-miniG(q) complex bound to clozapine-N-oxide; and a hM3R-miniG(q) complex bound to iperoxo. Complemented with mutagenesis, functional and computational simulation data, our structures reveal key details of the recognition of DREADD chemogenetic actuators and the molecular basis for activation. These findings should accelerate the structure-guided discovery of next-generation chemogenetic tools.

			Molecular basis for selective activation of DREADD-based chemogenetics.,Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL Nature. 2022 Dec;612(7939):354-362. doi: 10.1038/s41586-022-05489-0. Epub 2022 , Nov 30. PMID:36450989<ref>PMID:36450989</ref>

			From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
			</div>
			<div class="pdbe-citations 8ea0" style="background-color:#fffaf0;"></div>

			==See Also==
			*[[Muscarinic acetylcholine receptor\|Muscarinic acetylcholine receptor]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 10:47, 30 November 2022

2022-11-30T10:47:03Z

← Older revision		Revision as of 10:47, 30 November 2022
Line 1:		Line 1:
	~~'''Unreleased structure'''~~

	~~The~~ entry ~~8ea0~~ is ~~ON HOLD until Paper Publication~~		==CryoEM structure of miniGq-coupled hM3R in complex with iperoxo (local refinement)==
			<StructureSection load='8ea0' size='340' side='right'caption='[[8ea0]], [[Resolution\|resolution]] 2.56Å' scene=''>
	~~Authors~~:		== Structural highlights ==
			<table><tr><td colspan='2'>[[8ea0]] is a 1 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=8EA0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8EA0 FirstGlance]. <br>
	~~Description~~:		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=IXO:4-(4,5-DIHYDRO-1,2-OXAZOL-3-YLOXY)-N,N,N-TRIMETHYLBUT-2-YN-1-AMINIUM'>IXO</scene>, <scene name='pdbligand=Y01:CHOLESTEROL+HEMISUCCINATE'>Y01</scene></td></tr>
	[[Category: ~~Unreleased~~ Structures]]		<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8ea0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8ea0 OCA], [https://pdbe.org/8ea0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8ea0 RCSB], [https://www.ebi.ac.uk/pdbsum/8ea0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8ea0 ProSAT]</span></td></tr>
			</table>
			== Disease ==
			[https://www.uniprot.org/uniprot/ACM3_HUMAN ACM3_HUMAN] Defects in CHRM3 are the cause of Eagle-Barrett syndrome (EGBRS) [MIM:[https://omim.org/entry/100100 100100]. EGBRS is a syndrome characterized by thin abdominal musculature with overlying lax skin, cryptorchism, megacystis with disorganized detrusor muscle, and urinary tract abnormalities.<ref>PMID:22077972</ref>
			== Function ==
			[https://www.uniprot.org/uniprot/ACM3_HUMAN ACM3_HUMAN] The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
			== References ==
			<references/>
			__TOC__
			</StructureSection>
			[[Category: Homo sapiens]]
			[[Category: Large Structures]]
			[[Category: Fay JF]]
			[[Category: Roth BL]]
			[[Category: Zhang S]]

OCA at 05:46, 14 September 2022

2022-09-14T05:46:53Z

← Older revision		Revision as of 05:46, 14 September 2022
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

	The entry 8ea0 is ON HOLD		The entry 8ea0 is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "8ea0" [edit=sysop:move=sysop]

2022-09-07T15:34:52Z

Protected "8ea0" [edit=sysop:move=sysop]

← Older revision	Revision as of 15:34, 7 September 2022
(No difference)

OCA: New page: '''Unreleased structure''' The entry 8ea0 is ON HOLD Authors: Description: Category: Unreleased Structures

2022-09-07T15:34:51Z

New page: '''Unreleased structure''' The entry 8ea0 is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 8ea0 is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]