6rv2 - Revision history

OCA at 12:29, 24 January 2024

OCA — Wed, 24 Jan 2024 12:29:26 GMT

←Older revision		Revision as of 12:29, 24 January 2024
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	<StructureSection load='6rv2' size='340' side='right'caption='[[6rv2]], [[Resolution\|resolution]] 3.00Å' scene=''>		<StructureSection load='6rv2' size='340' side='right'caption='[[6rv2]], [[Resolution\|resolution]] 3.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6rv2]] is a 4 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6RV2 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=6RV2 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6rv2]] is a 4 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=6RV2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6RV2 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DMU:DECYL-BETA-D-MALTOPYRANOSIDE'>DMU</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene>, <scene name='pdbligand=PC1:1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>PC1</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">X-ray diffraction, [[Resolution\|Resolution]] 3Å</td></tr>
-	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">KCNK3, TASK, TASK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])~~</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DMU:DECYL-BETA-D-MALTOPYRANOSIDE'>DMU</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene>, <scene name='pdbligand=PC1:1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>PC1</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'>[~~http~~://proteopedia.org/fgij/fg.htm?mol=6rv2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6rv2 OCA], [~~http~~://pdbe.org/6rv2 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=6rv2 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/6rv2 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=6rv2 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=6rv2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6rv2 OCA], [https://pdbe.org/6rv2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6rv2 RCSB], [https://www.ebi.ac.uk/pdbsum/6rv2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6rv2 ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
-	[~~[http~~://www.uniprot.org/uniprot/KCNK3_HUMAN KCNK3_HUMAN]] Heritable pulmonary arterial hypertension. The disease is caused by mutations affecting the gene represented in this entry.	+	[https://www.uniprot.org/uniprot/KCNK3_HUMAN KCNK3_HUMAN] Heritable pulmonary arterial hypertension. The disease is caused by mutations affecting the gene represented in this entry.
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/KCNK3_HUMAN KCNK3_HUMAN]] pH-dependent, voltage-insensitive, background potassium channel protein. Rectification direction results from potassium ion concentration on either side of the membrane. Acts as an outward rectifier when external potassium concentration is low. When external potassium concentration is high, current is inward.<ref>PMID:23169818</ref> <ref>PMID:9312005</ref>	+	[https://www.uniprot.org/uniprot/KCNK3_HUMAN KCNK3_HUMAN] pH-dependent, voltage-insensitive, background potassium channel protein. Rectification direction results from potassium ion concentration on either side of the membrane. Acts as an outward rectifier when external potassium concentration is low. When external potassium concentration is high, current is inward.<ref>PMID:23169818</ref> <ref>PMID:9312005</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Arrowsmith~~, C H~~]]	+	[[Category: Arrowsmith CH]]
-	[[Category: Bountra, C]]	+	[[Category: Bountra C]]
-	[[Category: Burgess-Brown, N]]	+	[[Category: Burgess-Brown N]]
-	[[Category: Bushell~~, S R~~]]	+	[[Category: Bushell SR]]
-	[[Category: Carpenter~~, E P~~]]	+	[[Category: Carpenter EP]]
-	[[Category: Chalk, R]]	+	[[Category: Chalk R]]
-	[[Category: Edwards~~, A M~~]]	+	[[Category: Edwards AM]]
-	[[Category: Mukhopadhyay~~, S M.M~~]]	+	[[Category: Mukhopadhyay SMM]]
-	[[Category: Pike~~, A C.W~~]]	+	[[Category: Pike ACW]]
-	[[Category: Quigley, A]]	+	[[Category: Quigley A]]
-	[[Category: Rodstrom~~, K E.J]]~~	+	[[Category: Rodstrom KEJ]]
-	~~[[Category: Structural genomic~~]]	+	[[Category: Shrestha L]]
-	[[Category: Shrestha, L]]	+	[[Category: Speedman D]]
-	[[Category: Speedman, D]]	+	[[Category: Tessitore A]]
-	[[Category: Tessitore, A]]	+	[[Category: Venkaya S]]
-	[[Category: Venkaya, S]]	+	[[Category: Zhang W]]
-	[[Category: Zhang, W]]	+
-	~~[[Category: Membrane protein]]~~	+
-	~~[[Category: Potassium channel]]~~	+
-	~~[[Category: Sgc~~]]	+

OCA at 11:26, 22 July 2020

OCA — Wed, 22 Jul 2020 11:26:22 GMT

←Older revision		Revision as of 11:26, 22 July 2020
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	<StructureSection load='6rv2' size='340' side='right'caption='[[6rv2]], [[Resolution\|resolution]] 3.00Å' scene=''>		<StructureSection load='6rv2' size='340' side='right'caption='[[6rv2]], [[Resolution\|resolution]] 3.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6rv2]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6RV2 OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6RV2 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6rv2]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6RV2 OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6RV2 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DMU:DECYL-BETA-D-MALTOPYRANOSIDE'>DMU</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene>, <scene name='pdbligand=PC1:1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>PC1</scene>, <scene name='pdbligand=Y01:CHOLESTEROL+HEMISUCCINATE'>Y01</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DMU:DECYL-BETA-D-MALTOPYRANOSIDE'>DMU</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene>, <scene name='pdbligand=PC1:1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>PC1</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'>[http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6rv2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6rv2 OCA], [http://pdbe.org/6rv2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6rv2 RCSB], [http://www.ebi.ac.uk/pdbsum/6rv2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6rv2 ProSAT]</span></td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">KCNK3, TASK, TASK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
		+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6rv2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6rv2 OCA], [http://pdbe.org/6rv2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6rv2 RCSB], [http://www.ebi.ac.uk/pdbsum/6rv2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6rv2 ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
Line 11:		Line 12:
	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/KCNK3_HUMAN KCNK3_HUMAN]] pH-dependent, voltage-insensitive, background potassium channel protein. Rectification direction results from potassium ion concentration on either side of the membrane. Acts as an outward rectifier when external potassium concentration is low. When external potassium concentration is high, current is inward.<ref>PMID:23169818</ref> <ref>PMID:9312005</ref>		[[http://www.uniprot.org/uniprot/KCNK3_HUMAN KCNK3_HUMAN]] pH-dependent, voltage-insensitive, background potassium channel protein. Rectification direction results from potassium ion concentration on either side of the membrane. Acts as an outward rectifier when external potassium concentration is low. When external potassium concentration is high, current is inward.<ref>PMID:23169818</ref> <ref>PMID:9312005</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	TWIK-related acid-sensitive potassium (TASK) channels-members of the two pore domain potassium (K2P) channel family-are found in neurons(1), cardiomyocytes(2-4) and vascular smooth muscle cells(5), where they are involved in the regulation of heart rate(6), pulmonary artery tone(5,7), sleep/wake cycles(8) and responses to volatile anaesthetics(8-11). K2P channels regulate the resting membrane potential, providing background K(+) currents controlled by numerous physiological stimuli(12-15). Unlike other K2P channels, TASK channels are able to bind inhibitors with high affinity, exceptional selectivity and very slow compound washout rates. As such, these channels are attractive drug targets, and TASK-1 inhibitors are currently in clinical trials for obstructive sleep apnoea and atrial fibrillation(16). In general, potassium channels have an intramembrane vestibule with a selectivity filter situated above and a gate with four parallel helices located below; however, the K2P channels studied so far all lack a lower gate. Here we present the X-ray crystal structure of TASK-1, and show that it contains a lower gate-which we designate as an 'X-gate'-created by interaction of the two crossed C-terminal M4 transmembrane helices at the vestibule entrance. This structure is formed by six residues ((243)VLRFMT(248)) that are essential for responses to volatile anaesthetics(10), neurotransmitters(13) and G-protein-coupled receptors(13). Mutations within the X-gate and the surrounding regions markedly affect both the channel-open probability and the activation of the channel by anaesthetics. Structures of TASK-1 bound to two high-affinity inhibitors show that both compounds bind below the selectivity filter and are trapped in the vestibule by the X-gate, which explains their exceptionally low washout rates. The presence of the X-gate in TASK channels explains many aspects of their physiological and pharmacological behaviour, which will be beneficial for the future development and optimization of TASK modulators for the treatment of heart, lung and sleep disorders.
		+
		+	A lower X-gate in TASK channels traps inhibitors within the vestibule.,Rodstrom KEJ, Kiper AK, Zhang W, Rinne S, Pike ACW, Goldstein M, Conrad LJ, Delbeck M, Hahn MG, Meier H, Platzk M, Quigley A, Speedman D, Shrestha L, Mukhopadhyay SMM, Burgess-Brown NA, Tucker SJ, Muller T, Decher N, Carpenter EP Nature. 2020 Jun;582(7812):443-447. doi: 10.1038/s41586-020-2250-8. Epub 2020 Apr, 29. PMID:32499642<ref>PMID:32499642</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 6rv2" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Potassium channel 3D structures\|Potassium channel 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Arrowsmith, C H]]		[[Category: Arrowsmith, C H]]

OCA at 06:06, 7 August 2019

OCA — Wed, 07 Aug 2019 06:06:21 GMT

←Older revision		Revision as of 06:06, 7 August 2019
Line 1:		Line 1:
-	'''Unreleased structure'''

-	The entry ~~6rv2~~ is ~~ON HOLD~~ ~~until Paper Publication~~	+	==Crystal structure of the human two pore domain potassium ion channel TASK-1 (K2P3.1) in a closed conformation==
-		+	<StructureSection load='6rv2' size='340' side='right'caption='[[6rv2]], [[Resolution\|resolution]] 3.00Å' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[6rv2]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6RV2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6RV2 FirstGlance]. <br>
-	~~Description~~:	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DMU:DECYL-BETA-D-MALTOPYRANOSIDE'>DMU</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene>, <scene name='pdbligand=PC1:1,2-DIACYL-SN-GLYCERO-3-PHOSPHOCHOLINE'>PC1</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'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6rv2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6rv2 OCA], [http://pdbe.org/6rv2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6rv2 RCSB], [http://www.ebi.ac.uk/pdbsum/6rv2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6rv2 ProSAT]</span></td></tr>
		+	</table>
		+	== Disease ==
		+	[[http://www.uniprot.org/uniprot/KCNK3_HUMAN KCNK3_HUMAN]] Heritable pulmonary arterial hypertension. The disease is caused by mutations affecting the gene represented in this entry.
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/KCNK3_HUMAN KCNK3_HUMAN]] pH-dependent, voltage-insensitive, background potassium channel protein. Rectification direction results from potassium ion concentration on either side of the membrane. Acts as an outward rectifier when external potassium concentration is low. When external potassium concentration is high, current is inward.<ref>PMID:23169818</ref> <ref>PMID:9312005</ref>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Arrowsmith, C H]]
		+	[[Category: Bountra, C]]
		+	[[Category: Burgess-Brown, N]]
		+	[[Category: Bushell, S R]]
		+	[[Category: Carpenter, E P]]
		+	[[Category: Chalk, R]]
		+	[[Category: Edwards, A M]]
		+	[[Category: Mukhopadhyay, S M.M]]
		+	[[Category: Pike, A C.W]]
		+	[[Category: Quigley, A]]
		+	[[Category: Rodstrom, K E.J]]
		+	[[Category: Structural genomic]]
		+	[[Category: Shrestha, L]]
		+	[[Category: Speedman, D]]
		+	[[Category: Tessitore, A]]
		+	[[Category: Venkaya, S]]
		+	[[Category: Zhang, W]]
		+	[[Category: Membrane protein]]
		+	[[Category: Potassium channel]]
		+	[[Category: Sgc]]

OCA at 04:21, 10 July 2019

OCA — Wed, 10 Jul 2019 04:21:26 GMT

←Older revision		Revision as of 04:21, 10 July 2019
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6rv2 is ON HOLD	+	The entry 6rv2 is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "6rv2" [edit=sysop:move=sysop]

OCA — Wed, 12 Jun 2019 04:11:31 GMT

Protected "6rv2" [edit=sysop:move=sysop]

←Older revision

Revision as of 04:11, 12 June 2019

OCA: New page: '''Unreleased structure''' The entry 6rv2 is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 12 Jun 2019 04:11:29 GMT

New page: '''Unreleased structure''' The entry 6rv2 is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 6rv2 is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]