OCA at 07:04, 18 May 2023

OCA — Thu, 18 May 2023 07:04:56 GMT

←Older revision		Revision as of 07:04, 18 May 2023
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-	'''Unreleased structure'''

-	~~The entry~~ 8sia is ~~ON HOLD until Paper~~ Publication	+	==Cryo-EM structure of TRPM7 N1098Q mutant in GDN detergent in complex with inhibitor NS8593 in closed state==
		+	<StructureSection load='8sia' size='340' side='right'caption='[[8sia]], [[Resolution\|resolution]] 2.91Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[8sia]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8SIA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8SIA FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6RA:N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl]-1H-benzimidazol-2-amine'>6RA</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=DU0:2-[2-[(1~{S},2~{S},4~{S},5~{R},6~{R},7~{S},8~{R},9~{S},12~{S},13~{R},16~{S})-5,7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icos-18-ene-6,2-oxane]-16-yl]oxyethyl]propane-1,3-diol'>DU0</scene>, <scene name='pdbligand=POV:(2S)-3-(HEXADECANOYLOXY)-2-[(9Z)-OCTADEC-9-ENOYLOXY]PROPYL+2-(TRIMETHYLAMMONIO)ETHYL+PHOSPHATE'>POV</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=8sia FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8sia OCA], [https://pdbe.org/8sia PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8sia RCSB], [https://www.ebi.ac.uk/pdbsum/8sia PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8sia ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[https://www.uniprot.org/uniprot/TRPM7_MOUSE TRPM7_MOUSE] Essential ion channel and serine/threonine-protein kinase. Divalent cation channel permeable to calcium and magnesium. Has a central role in magnesium ion homeostasis and in the regulation of anoxic neuronal cell death. The kinase activity is essential for the channel function. May be involved in a fundamental process that adjusts plasma membrane divalent cation fluxes according to the metabolic state of the cell. Phosphorylates annexin A1 (ANXA1).<ref>PMID:11385574</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The transient receptor potential channel TRPM7 is a master regulator of the organismal balance of divalent cations that plays an essential role in embryonic development, immune responses, cell mobility, proliferation, and differentiation. TRPM7 is implicated in neuronal and cardiovascular disorders, tumor progression and has emerged as a new drug target. Here we use cryo-EM, functional analysis, and molecular dynamics simulations to uncover two distinct structural mechanisms of TRPM7 activation by a gain-of-function mutation and by the agonist naltriben, which show different conformational dynamics and domain involvement. We identify a binding site for highly potent and selective inhibitors and show that they act by stabilizing the TRPM7 closed state. The discovered structural mechanisms provide foundations for understanding the molecular basis of TRPM7 channelopathies and drug development.

-	~~Authors~~:	+	Structural mechanisms of TRPM7 activation and inhibition.,Nadezhdin KD, Correia L, Narangoda C, Patel DS, Neuberger A, Gudermann T, Kurnikova MG, Chubanov V, Sobolevsky AI Nat Commun. 2023 May 8;14(1):2639. doi: 10.1038/s41467-023-38362-3. PMID:37156763<ref>PMID:37156763</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased~~ Structures]]	+	</div>
		+	<div class="pdbe-citations 8sia" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Mus musculus]]
		+	[[Category: Nadezhdin KD]]
		+	[[Category: Neuberger A]]
		+	[[Category: Sobolevsky AI]]

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

OCA — Wed, 26 Apr 2023 15:25:31 GMT

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

←Older revision

Revision as of 15:25, 26 April 2023

OCA: New page: '''Unreleased structure''' The entry 8sia is ON HOLD until Paper Publication Authors: Description: Category: Unreleased Structures

OCA — Wed, 26 Apr 2023 15:25:30 GMT

New page: '''Unreleased structure''' The entry 8sia is ON HOLD until Paper Publication Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 8sia is ON HOLD until Paper Publication

Authors:

Description:
[[Category: Unreleased Structures]]

8sia - Revision history

OCA at 07:04, 18 May 2023

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

OCA: New page: '''Unreleased structure''' The entry 8sia is ON HOLD until Paper Publication Authors: Description: Category: Unreleased Structures