8i5g - Revision history

OCA at 17:01, 8 November 2023

OCA — Wed, 08 Nov 2023 17:01:51 GMT

←Older revision		Revision as of 17:01, 8 November 2023
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	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[8i5g]] is a 3 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=8I5G OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8I5G FirstGlance]. <br>		<table><tr><td colspan='2'>[[8i5g]] is a 3 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=8I5G OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8I5G FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=9Z9:(3beta,14beta,17beta,25R)-3-[4-methoxy-3-(methoxymethyl)butoxy]spirost-5-en'>9Z9</scene>, <scene name='pdbligand=LPE:1-O-OCTADECYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>LPE</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=PCW:1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>PCW</scene>, <scene name='pdbligand=T70:4-[2-(5-azanyl-1~{H}-pyrazol-4-yl)-4-chloranyl-phenoxy]-5-chloranyl-2-fluoranyl-~{N}-(1,3-thiazol-4-yl)benzenesulfonamide'>T70</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]] 2.7Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=9Z9:(3beta,14beta,17beta,25R)-3-[4-methoxy-3-(methoxymethyl)butoxy]spirost-5-en'>9Z9</scene>, <scene name='pdbligand=LPE:1-O-OCTADECYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>LPE</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=PCW:1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>PCW</scene>, <scene name='pdbligand=T70:4-[2-(5-azanyl-1~{H}-pyrazol-4-yl)-4-chloranyl-phenoxy]-5-chloranyl-2-fluoranyl-~{N}-(1,3-thiazol-4-yl)benzenesulfonamide'>T70</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=8i5g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8i5g OCA], [https://pdbe.org/8i5g PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8i5g RCSB], [https://www.ebi.ac.uk/pdbsum/8i5g PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8i5g 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=8i5g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8i5g OCA], [https://pdbe.org/8i5g PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8i5g RCSB], [https://www.ebi.ac.uk/pdbsum/8i5g PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8i5g ProSAT]</span></td></tr>
	</table>		</table>

OCA at 08:20, 14 June 2023

OCA — Wed, 14 Jun 2023 08:20:20 GMT

←Older revision		Revision as of 08:20, 14 June 2023
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-	'''Unreleased structure'''

-	The entry ~~8i5g~~ is ~~ON HOLD~~ ~~until Paper~~ Publication	+	==Structure of human Nav1.7 in complex with PF-05089771==
		+	<StructureSection load='8i5g' size='340' side='right'caption='[[8i5g]], [[Resolution\|resolution]] 2.70Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[8i5g]] is a 3 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=8I5G OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8I5G FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=9Z9:(3beta,14beta,17beta,25R)-3-[4-methoxy-3-(methoxymethyl)butoxy]spirost-5-en'>9Z9</scene>, <scene name='pdbligand=LPE:1-O-OCTADECYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>LPE</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=PCW:1,2-DIOLEOYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>PCW</scene>, <scene name='pdbligand=T70:4-[2-(5-azanyl-1~{H}-pyrazol-4-yl)-4-chloranyl-phenoxy]-5-chloranyl-2-fluoranyl-~{N}-(1,3-thiazol-4-yl)benzenesulfonamide'>T70</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=8i5g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8i5g OCA], [https://pdbe.org/8i5g PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8i5g RCSB], [https://www.ebi.ac.uk/pdbsum/8i5g PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8i5g ProSAT]</span></td></tr>
		+	</table>
		+	== Disease ==
		+	[https://www.uniprot.org/uniprot/SCN1B_HUMAN SCN1B_HUMAN] Dravet syndrome;Familial progressive cardiac conduction defect;Generalized epilepsy with febrile seizures-plus;Brugada syndrome. The disease is caused by mutations affecting the gene represented in this entry. The gene represented in this entry may be involved in disease pathogenesis. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry.
		+	== Function ==
		+	[https://www.uniprot.org/uniprot/SCN1B_HUMAN SCN1B_HUMAN] Crucial in the assembly, expression, and functional modulation of the heterotrimeric complex of the sodium channel. The subunit beta-1 can modulate multiple alpha subunit isoforms from brain, skeletal muscle, and heart. Its association with NFASC may target the sodium channels to the nodes of Ranvier of developing axons and retain these channels at the nodes in mature myelinated axons.<ref>PMID:14622265</ref> Isoform 2: Cell adhesion molecule that plays a critical role in neuronal migration and pathfinding during brain development. Stimulates neurite outgrowth.<ref>PMID:14622265</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Voltage-gated sodium (Na(v)) channels are targeted by a number of widely used and investigational drugs for the treatment of epilepsy, arrhythmia, pain, and other disorders. Despite recent advances in structural elucidation of Na(v) channels, the binding mode of most Na(v)-targeting drugs remains unknown. Here we report high-resolution cryo-EM structures of human Na(v)1.7 treated with drugs and lead compounds with representative chemical backbones at resolutions of 2.6-3.2 A. A binding site beneath the intracellular gate (site BIG) accommodates carbamazepine, bupivacaine, and lacosamide. Unexpectedly, a second molecule of lacosamide plugs into the selectivity filter from the central cavity. Fenestrations are popular sites for various state-dependent drugs. We show that vinpocetine, a synthetic derivative of a vinca alkaloid, and hardwickiic acid, a natural product with antinociceptive effect, bind to the III-IV fenestration, while vixotrigine, an analgesic candidate, penetrates the IV-I fenestration of the pore domain. Our results permit building a 3D structural map for known drug-binding sites on Na(v) channels summarized from the present and previous structures.

-	~~Authors~~:	+	Structural mapping of Na(v)1.7 antagonists.,Wu Q, Huang J, Fan X, Wang K, Jin X, Huang G, Li J, Pan X, Yan N Nat Commun. 2023 Jun 3;14(1):3224. doi: 10.1038/s41467-023-38942-3. PMID:37270609<ref>PMID:37270609</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased~~ Structures]]	+	</div>
		+	<div class="pdbe-citations 8i5g" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Homo sapiens]]
		+	[[Category: Large Structures]]
		+	[[Category: Wu QR]]
		+	[[Category: Yan N]]

OCA at 02:20, 25 May 2023

OCA — Thu, 25 May 2023 02:20:36 GMT

←Older revision		Revision as of 02:20, 25 May 2023
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 8i5g is ON HOLD	+	The entry 8i5g is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "8i5g" [edit=sysop:move=sysop]

OCA — Wed, 01 Feb 2023 09:38:51 GMT

Protected "8i5g" [edit=sysop:move=sysop]

←Older revision

Revision as of 09:38, 1 February 2023

OCA: New page: '''Unreleased structure''' The entry 8i5g is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 01 Feb 2023 09:38:50 GMT

New page: '''Unreleased structure''' The entry 8i5g is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 8i5g is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]