6d7q - Revision history

OCA at 15:19, 4 October 2023

OCA — Wed, 04 Oct 2023 15:19:37 GMT

←Older revision		Revision as of 15:19, 4 October 2023
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	<StructureSection load='6d7q' size='340' side='right'caption='[[6d7q]], [[Resolution\|resolution]] 3.50Å' scene=''>		<StructureSection load='6d7q' size='340' side='right'caption='[[6d7q]], [[Resolution\|resolution]] 3.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6d7q]] is a 1 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Buffalo_rat Buffalo rat~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D7Q OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6D7Q FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6d7q]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D7Q OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6D7Q FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=DTB:6-(5-METHYL-2-OXO-IMIDAZOLIDIN-4-YL)-HEXANOIC+ACID'>DTB</scene>, <scene name='pdbligand=FZ4:2-aminoethyl+diphenylborinate'>FZ4</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]] 3.497Å</td></tr>
-	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Trpv6 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat])~~</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=DTB:6-(5-METHYL-2-OXO-IMIDAZOLIDIN-4-YL)-HEXANOIC+ACID'>DTB</scene>, <scene name='pdbligand=FZ4:2-aminoethyl+diphenylborinate'>FZ4</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=6d7q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d7q OCA], [~~http~~://pdbe.org/6d7q PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=6d7q RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/6d7q PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=6d7q 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=6d7q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d7q OCA], [https://pdbe.org/6d7q PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6d7q RCSB], [https://www.ebi.ac.uk/pdbsum/6d7q PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6d7q ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/TRPV6_RAT TRPV6_RAT]] Calcium selective cation channel probably involved in Ca(2+) uptake in various tissues, including Ca(2+) reabsorption in intestine. The channel is activated by low internal calcium level, probably including intracellular calcium store depletion, and the current exhibits an inward rectification. Inactivation includes both, a rapid Ca(2+)-dependent and a slower Ca(2+)-calmodulin-dependent mechanism, the latter may be regulated by phosphorylation. In vitro, is slowly inhibited by Mg(2+) in a voltage-independent manner. Heteromeric assembly with TRPV5 seems to modify channel properties. TRPV5-TRPV6 heteromultimeric concatemers exhibit voltage-dependent gating (By similarity).[UniProtKB:Q91WD2][UniProtKB:Q9H1D0]<ref>PMID:11287959</ref>	+	[https://www.uniprot.org/uniprot/TRPV6_RAT TRPV6_RAT] Calcium selective cation channel probably involved in Ca(2+) uptake in various tissues, including Ca(2+) reabsorption in intestine. The channel is activated by low internal calcium level, probably including intracellular calcium store depletion, and the current exhibits an inward rectification. Inactivation includes both, a rapid Ca(2+)-dependent and a slower Ca(2+)-calmodulin-dependent mechanism, the latter may be regulated by phosphorylation. In vitro, is slowly inhibited by Mg(2+) in a voltage-independent manner. Heteromeric assembly with TRPV5 seems to modify channel properties. TRPV5-TRPV6 heteromultimeric concatemers exhibit voltage-dependent gating (By similarity).[UniProtKB:Q91WD2][UniProtKB:Q9H1D0]<ref>PMID:11287959</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	</div>		</div>
	<div class="pdbe-citations 6d7q" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 6d7q" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Ion channels 3D structures\|Ion channels 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: Buffalo rat]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~McGoldrick, L L~~]]	+	[[Category: Rattus norvegicus]]
-	[[Category: ~~Saotome, K~~]]	+	[[Category: McGoldrick LL]]
-	[[Category: ~~Singh, A~~ K]]	+	[[Category: Saotome K]]
-	[[Category: ~~Sobolevsky, A I~~]]	+	[[Category: Singh AK]]
-	[[Category: ~~Calcium channel]]~~	+	[[Category: Sobolevsky AI]]
-	~~[[Category: Epithelial calcium channel]]~~	+
-	~~[[Category: Ion channel]]~~	+
-	~~[[Category: Membrane protein]]~~	+
-	~~[[Category: Membrane protein-inhibitor complex]]~~	+
-	~~[[Category: Transporter~~]]	+

OCA at 10:00, 18 December 2019

OCA — Wed, 18 Dec 2019 10:00:06 GMT

←Older revision		Revision as of 10:00, 18 December 2019
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	==Crystal Structure of Rat TRPV6*-Y466A in complex with 2-Aminoethoxydiphenyl borate (2-APB)==		==Crystal Structure of Rat TRPV6*-Y466A in complex with 2-Aminoethoxydiphenyl borate (2-APB)==
-	<StructureSection load='6d7q' size='340' side='right' caption='[[6d7q]], [[Resolution\|resolution]] 3.50Å' scene=''>	+	<StructureSection load='6d7q' size='340' side='right'caption='[[6d7q]], [[Resolution\|resolution]] 3.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6d7q]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D7Q OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D7Q FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6d7q]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Buffalo_rat Buffalo rat]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D7Q OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D7Q FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=DTB:6-(5-METHYL-2-OXO-IMIDAZOLIDIN-4-YL)-HEXANOIC+ACID'>DTB</scene>, <scene name='pdbligand=FZ4:2-aminoethyl+diphenylborinate'>FZ4</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=DTB:6-(5-METHYL-2-OXO-IMIDAZOLIDIN-4-YL)-HEXANOIC+ACID'>DTB</scene>, <scene name='pdbligand=FZ4:2-aminoethyl+diphenylborinate'>FZ4</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Trpv6 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat])</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=6d7q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d7q OCA], [http://pdbe.org/6d7q PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d7q RCSB], [http://www.ebi.ac.uk/pdbsum/6d7q PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d7q ProSAT]</span></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=6d7q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d7q OCA], [http://pdbe.org/6d7q PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d7q RCSB], [http://www.ebi.ac.uk/pdbsum/6d7q PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d7q ProSAT]</span></td></tr>
	</table>		</table>
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Buffalo rat]]
		+	[[Category: Large Structures]]
	[[Category: McGoldrick, L L]]		[[Category: McGoldrick, L L]]
	[[Category: Saotome, K]]		[[Category: Saotome, K]]

OCA at 07:37, 18 July 2018

OCA — Wed, 18 Jul 2018 07:37:17 GMT

←Older revision		Revision as of 07:37, 18 July 2018
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 6d7q is ~~ON HOLD~~ ~~until Paper~~ Publication	+	==Crystal Structure of Rat TRPV6*-Y466A in complex with 2-Aminoethoxydiphenyl borate (2-APB)==
		+	<StructureSection load='6d7q' size='340' side='right' caption='[[6d7q]], [[Resolution\|resolution]] 3.50Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[6d7q]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D7Q OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D7Q FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=DTB:6-(5-METHYL-2-OXO-IMIDAZOLIDIN-4-YL)-HEXANOIC+ACID'>DTB</scene>, <scene name='pdbligand=FZ4:2-aminoethyl+diphenylborinate'>FZ4</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=6d7q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d7q OCA], [http://pdbe.org/6d7q PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d7q RCSB], [http://www.ebi.ac.uk/pdbsum/6d7q PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d7q ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/TRPV6_RAT TRPV6_RAT]] Calcium selective cation channel probably involved in Ca(2+) uptake in various tissues, including Ca(2+) reabsorption in intestine. The channel is activated by low internal calcium level, probably including intracellular calcium store depletion, and the current exhibits an inward rectification. Inactivation includes both, a rapid Ca(2+)-dependent and a slower Ca(2+)-calmodulin-dependent mechanism, the latter may be regulated by phosphorylation. In vitro, is slowly inhibited by Mg(2+) in a voltage-independent manner. Heteromeric assembly with TRPV5 seems to modify channel properties. TRPV5-TRPV6 heteromultimeric concatemers exhibit voltage-dependent gating (By similarity).[UniProtKB:Q91WD2][UniProtKB:Q9H1D0]<ref>PMID:11287959</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Transient receptor potential (TRP) channels are involved in various physiological processes, including sensory transduction. The TRP channel TRPV6 mediates calcium uptake in epithelia and its expression is dramatically increased in numerous types of cancer. TRPV6 inhibitors suppress tumor growth, but the molecular mechanism of inhibition remains unknown. Here, we present crystal and cryo-EM structures of human and rat TRPV6 bound to 2-aminoethoxydiphenyl borate (2-APB), a TRPV6 inhibitor and modulator of numerous TRP channels. 2-APB binds to TRPV6 in a pocket formed by the cytoplasmic half of the S1-S4 transmembrane helix bundle. Comparing human wild-type and high-affinity mutant Y467A structures, we show that 2-APB induces TRPV6 channel closure by modulating protein-lipid interactions. Mutagenesis and functional analyses suggest that the identified 2-APB binding site might be present in other members of vanilloid subfamily TRP channels. Our findings reveal a mechanism of ion channel allosteric modulation that can be exploited for therapeutic design.

-	~~Authors~~:	+	Structural bases of TRP channel TRPV6 allosteric modulation by 2-APB.,Singh AK, Saotome K, McGoldrick LL, Sobolevsky AI Nat Commun. 2018 Jun 25;9(1):2465. doi: 10.1038/s41467-018-04828-y. PMID:29941865<ref>PMID:29941865</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
		+	<div class="pdbe-citations 6d7q" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: McGoldrick, L L]]
		+	[[Category: Saotome, K]]
		+	[[Category: Singh, A K]]
		+	[[Category: Sobolevsky, A I]]
		+	[[Category: Calcium channel]]
		+	[[Category: Epithelial calcium channel]]
		+	[[Category: Ion channel]]
		+	[[Category: Membrane protein]]
		+	[[Category: Membrane protein-inhibitor complex]]
		+	[[Category: Transporter]]

OCA at 04:01, 16 May 2018

OCA — Wed, 16 May 2018 04:01:54 GMT

←Older revision		Revision as of 04:01, 16 May 2018
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6d7q is ON HOLD	+	The entry 6d7q is ON HOLD until Paper Publication

	Authors:		Authors:

OCA at 04:50, 9 May 2018

OCA — Wed, 09 May 2018 04:50:04 GMT

←Older revision		Revision as of 04:50, 9 May 2018
Line 3:		Line 3:
	The entry 6d7q is ON HOLD		The entry 6d7q is ON HOLD

-	Authors: ~~Singh, A.K., Saotome, K., McGoldrick, L.L., Sobolevsky, A.I.~~	+	Authors:

-	Description: ~~Crystal Structure of Rat TRPV6*-Y466A in complex with 2-Aminoethoxydiphenyl borate (2-APB)~~	+	Description:
	[[Category: Unreleased Structures]]		[[Category: Unreleased Structures]]
-	[[Category: Sobolevsky, A.I]]
-	[[Category: Saotome, K]]
-	[[Category: Mcgoldrick, L.L]]
-	[[Category: Singh, A.K]]

OCA: Protected "6d7q" [edit=sysop:move=sysop]

OCA — Wed, 02 May 2018 06:47:43 GMT

Protected "6d7q" [edit=sysop:move=sysop]

←Older revision

Revision as of 06:47, 2 May 2018

OCA: New page: '''Unreleased structure''' The entry 6d7q is ON HOLD Authors: Singh, A.K., Saotome, K., McGoldrick, L.L., Sobolevsky, A.I. Description: Crystal Structure of Rat TRPV6*-Y466A in complex...

OCA — Wed, 02 May 2018 06:47:42 GMT

New page: '''Unreleased structure''' The entry 6d7q is ON HOLD Authors: Singh, A.K., Saotome, K., McGoldrick, L.L., Sobolevsky, A.I. Description: Crystal Structure of Rat TRPV6*-Y466A in complex...

New page

'''Unreleased structure'''

The entry 6d7q is ON HOLD

Authors: Singh, A.K., Saotome, K., McGoldrick, L.L., Sobolevsky, A.I.

Description: Crystal Structure of Rat TRPV6*-Y466A in complex with 2-Aminoethoxydiphenyl borate (2-APB)
[[Category: Unreleased Structures]]
[[Category: Sobolevsky, A.I]]
[[Category: Saotome, K]]
[[Category: Mcgoldrick, L.L]]
[[Category: Singh, A.K]]