6d7t - Revision history

OCA at 23:58, 10 April 2020

OCA — Fri, 10 Apr 2020 23:58:01 GMT

←Older revision		Revision as of 23:58, 10 April 2020
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	<SX load='6d7t' size='340' side='right' viewer='molstar' caption='[[6d7t]], [[Resolution\|resolution]] 4.44Å' scene=''>		<SX load='6d7t' size='340' side='right' viewer='molstar' caption='[[6d7t]], [[Resolution\|resolution]] 4.44Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6d7t]] 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=6D7T OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6D7T FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6d7t]] 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=6D7T OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6D7T 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=FZ4:2-aminoethyl+diphenylborinate'>FZ4</scene></td></tr>	+	</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=FZ4:2-aminoethyl+diphenylborinate'>FZ4</scene></td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">TRPV6, ECAC2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">TRPV6, ECAC2 ([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://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6d7t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d7t OCA], [http://pdbe.org/6d7t PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d7t RCSB], [http://www.ebi.ac.uk/pdbsum/6d7t PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d7t ProSAT]</span></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=6d7t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d7t OCA], [http://pdbe.org/6d7t PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d7t RCSB], [http://www.ebi.ac.uk/pdbsum/6d7t PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d7t ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==

OCA at 20:51, 6 March 2020

OCA — Fri, 06 Mar 2020 20:51:46 GMT

←Older revision		Revision as of 20:51, 6 March 2020
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	==Cryo-EM structure of human TRPV6-Y467A in complex with 2-Aminoethoxydiphenyl borate (2-APB)==		==Cryo-EM structure of human TRPV6-Y467A in complex with 2-Aminoethoxydiphenyl borate (2-APB)==
-	<~~StructureSection~~ load='6d7t' size='340' side='right'caption='[[6d7t]], [[Resolution\|resolution]] 4.44Å' scene=''>	+	<SX load='6d7t' size='340' side='right' viewer='molstar' caption='[[6d7t]], [[Resolution\|resolution]] 4.44Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[6d7t]] 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=6D7T OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D7T FirstGlance]. <br>		<table><tr><td colspan='2'>[[6d7t]] 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=6D7T OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D7T FirstGlance]. <br>
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	<references/>		<references/>
	__TOC__		__TOC__
-	</~~StructureSection~~>	+	</SX>
	[[Category: Human]]		[[Category: Human]]
	[[Category: Large Structures]]		[[Category: Large Structures]]

OCA at 10:00, 18 December 2019

OCA — Wed, 18 Dec 2019 10:00:18 GMT

←Older revision		Revision as of 10:00, 18 December 2019
Line 1:		Line 1:

	==Cryo-EM structure of human TRPV6-Y467A in complex with 2-Aminoethoxydiphenyl borate (2-APB)==		==Cryo-EM structure of human TRPV6-Y467A in complex with 2-Aminoethoxydiphenyl borate (2-APB)==
-	<StructureSection load='6d7t' size='340' side='right' caption='[[6d7t]], [[Resolution\|resolution]] 4.44Å' scene=''>	+	<StructureSection load='6d7t' size='340' side='right'caption='[[6d7t]], [[Resolution\|resolution]] 4.44Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6d7t]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D7T OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D7T FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6d7t]] 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=6D7T OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D7T 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=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=FZ4:2-aminoethyl+diphenylborinate'>FZ4</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">TRPV6, ECAC2 ([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://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6d7t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d7t OCA], [http://pdbe.org/6d7t PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d7t RCSB], [http://www.ebi.ac.uk/pdbsum/6d7t PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d7t 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=6d7t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d7t OCA], [http://pdbe.org/6d7t PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d7t RCSB], [http://www.ebi.ac.uk/pdbsum/6d7t PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d7t ProSAT]</span></td></tr>
	</table>		</table>
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
		+	[[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 07:37:42 GMT

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

-	~~The entry~~ 6d7t is ~~ON HOLD~~	+	==Cryo-EM structure of human TRPV6-Y467A in complex with 2-Aminoethoxydiphenyl borate (2-APB)==
		+	<StructureSection load='6d7t' size='340' side='right' caption='[[6d7t]], [[Resolution\|resolution]] 4.44Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[6d7t]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D7T OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D7T 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=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=6d7t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d7t OCA], [http://pdbe.org/6d7t PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d7t RCSB], [http://www.ebi.ac.uk/pdbsum/6d7t PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d7t ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/TRPV6_HUMAN TRPV6_HUMAN]] Calcium selective cation channel that mediates Ca(2+) uptake in various tissues, including the intestine (PubMed:11097838, PubMed:11278579, PubMed:11248124 PubMed:15184369, PubMed:23612980). Important for normal Ca(2+) ion homeostasis in the body, including bone and skin (By similarity). The channel is activated by low internal calcium level, probably including intracellular calcium store depletion, and the current exhibits an inward rectification (PubMed:15184369). 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.[UniProtKB:Q91WD2]<ref>PMID:11097838</ref> <ref>PMID:11248124</ref> <ref>PMID:11278579</ref> <ref>PMID:15184369</ref> <ref>PMID:23612980</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 6d7t" 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: Transporter]]

OCA at 04:50, 9 May 2018

OCA — Wed, 09 May 2018 04:50:07 GMT

←Older revision		Revision as of 04:50, 9 May 2018
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	The entry 6d7t is ON HOLD		The entry 6d7t is ON HOLD

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

-	Description: ~~Cryo-EM structure of human TRPV6-Y467A 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 "6d7t" [edit=sysop:move=sysop]

OCA — Wed, 02 May 2018 06:48:09 GMT

Protected "6d7t" [edit=sysop:move=sysop]

←Older revision

Revision as of 06:48, 2 May 2018

OCA: New page: '''Unreleased structure''' The entry 6d7t is ON HOLD Authors: Singh, A.K., Saotome, K., McGoldrick, L.L., Sobolevsky, A.I. Description: Cryo-EM structure of human TRPV6-Y467A in comple...

OCA — Wed, 02 May 2018 06:48:08 GMT

New page: '''Unreleased structure''' The entry 6d7t is ON HOLD Authors: Singh, A.K., Saotome, K., McGoldrick, L.L., Sobolevsky, A.I. Description: Cryo-EM structure of human TRPV6-Y467A in comple...

New page

'''Unreleased structure'''

The entry 6d7t is ON HOLD

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

Description: Cryo-EM structure of human TRPV6-Y467A 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]]