5lga - Revision history

OCA at 08:59, 11 October 2023

2023-10-11T08:59:10Z

←Older revision		Revision as of 08:59, 11 October 2023
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	==Structural analysis and biological activities of BXL0124, a Gemini analog of Vitamin D==		==Structural analysis and biological activities of BXL0124, a Gemini analog of Vitamin D==
-	<StructureSection load='5lga' size='340' side='right' caption='[[5lga]], [[Resolution\|resolution]] 2.50Å' scene=''>	+	<StructureSection load='5lga' size='340' side='right'caption='[[5lga]], [[Resolution\|resolution]] 2.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5lga]] is a 2 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Brachidanio_rerio Brachidanio~~ rerio]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5LGA OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5LGA FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5lga]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Danio_rerio Danio rerio] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5LGA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5LGA FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6VH:(1~{R},3~{S},5~{Z})-5-[2-[(1~{R},3~{A}~{S},7~{A}~{R})-7~{A}-METHYL-1-[(6~{R})-1,1,1-TRIS(FLUORANYL)-10-METHYL-2,10-BIS(OXIDANYL)-2-(TRIFLUOROMETHYL)UNDECA-3,8-DIYN-6-YL]-2,3,3~{A},5,6,7-HEXAHYDRO-1~{H}-INDEN-4-YLIDENE]ETHYLIDENE]-4-METHYLIDENE-CYCLOHEXANE-1,3-DIOL'>6VH</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]] 2.5Å</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">vdra, nr1i1a, vdr ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=7955 Brachidanio rerio])</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6VH:(1~{R},3~{S},5~{Z})-5-[2-[(1~{R},3~{A}~{S},7~{A}~{R})-7~{A}-METHYL-1-[(6~{R})-1,1,1-TRIS(FLUORANYL)-10-METHYL-2,10-BIS(OXIDANYL)-2-(TRIFLUOROMETHYL)UNDECA-3,8-DIYN-6-YL]-2,3,3~{A},5,6,7-HEXAHYDRO-1~{H}-INDEN-4-YLIDENE]ETHYLIDENE]-4-METHYLIDENE-CYCLOHEXANE-1,3-DIOL'>6VH</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=5lga FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lga OCA], [~~http~~://pdbe.org/5lga PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5lga RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5lga PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5lga 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=5lga FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lga OCA], [https://pdbe.org/5lga PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5lga RCSB], [https://www.ebi.ac.uk/pdbsum/5lga PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5lga ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/VDRA_DANRE VDRA_DANRE]] Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Regulates transcription of hormone sensitive genes via its association with the WINAC complex, a chromatin-remodeling complex. Plays a central role in calcium homeostasis.<ref>PMID:17218092</ref>	+	[https://www.uniprot.org/uniprot/VDRA_DANRE VDRA_DANRE] Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Regulates transcription of hormone sensitive genes via its association with the WINAC complex, a chromatin-remodeling complex. Plays a central role in calcium homeostasis.<ref>PMID:17218092</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 5lga" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 5lga" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Vitamin D receptor 3D structures\|Vitamin D receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Brachidanio~~ rerio]]	+	[[Category: Danio rerio]]
-	[[Category: ~~Belorusova, A Y~~]]	+	[[Category: Homo sapiens]]
-	[[Category: ~~Rochel, N~~]]	+	[[Category: Large Structures]]
-	[[Category: ~~Agonist~~]]	+	[[Category: Belorusova AY]]
-	[[Category: ~~Gemini]]~~	+	[[Category: Rochel N]]
-	~~[[Category: Transcription]]~~	+
-	~~[[Category: Vitamin d nuclear receptor~~]]	+

OCA at 18:37, 15 November 2017

2017-11-15T18:37:30Z

←Older revision		Revision as of 18:37, 15 November 2017
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	<StructureSection load='5lga' size='340' side='right' caption='[[5lga]], [[Resolution\|resolution]] 2.50Å' scene=''>		<StructureSection load='5lga' size='340' side='right' caption='[[5lga]], [[Resolution\|resolution]] 2.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5lga]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5LGA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5LGA FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5lga]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Brachidanio_rerio Brachidanio rerio]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5LGA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5LGA FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6VH:(1~{R},3~{S},5~{Z})-5-[2-[(1~{R},3~{A}~{S},7~{A}~{R})-7~{A}-METHYL-1-[(6~{R})-1,1,1-TRIS(FLUORANYL)-10-METHYL-2,10-BIS(OXIDANYL)-2-(TRIFLUOROMETHYL)UNDECA-3,8-DIYN-6-YL]-2,3,3~{A},5,6,7-HEXAHYDRO-1~{H}-INDEN-4-YLIDENE]ETHYLIDENE]-4-METHYLIDENE-CYCLOHEXANE-1,3-DIOL'>6VH</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6VH:(1~{R},3~{S},5~{Z})-5-[2-[(1~{R},3~{A}~{S},7~{A}~{R})-7~{A}-METHYL-1-[(6~{R})-1,1,1-TRIS(FLUORANYL)-10-METHYL-2,10-BIS(OXIDANYL)-2-(TRIFLUOROMETHYL)UNDECA-3,8-DIYN-6-YL]-2,3,3~{A},5,6,7-HEXAHYDRO-1~{H}-INDEN-4-YLIDENE]ETHYLIDENE]-4-METHYLIDENE-CYCLOHEXANE-1,3-DIOL'>6VH</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">vdra, nr1i1a, vdr ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=7955 Brachidanio rerio])</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=5lga FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lga OCA], [http://pdbe.org/5lga PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5lga RCSB], [http://www.ebi.ac.uk/pdbsum/5lga PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5lga 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=5lga FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lga OCA], [http://pdbe.org/5lga PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5lga RCSB], [http://www.ebi.ac.uk/pdbsum/5lga PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5lga ProSAT]</span></td></tr>
	</table>		</table>
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Brachidanio rerio]]
	[[Category: Belorusova, A Y]]		[[Category: Belorusova, A Y]]
	[[Category: Rochel, N]]		[[Category: Rochel, N]]

OCA at 17:18, 19 October 2016

2016-10-19T17:18:02Z

←Older revision		Revision as of 17:18, 19 October 2016
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-	'''Unreleased structure'''

-	~~The entry~~ 5lga is ~~ON HOLD~~ ~~until Paper~~ Publication	+	==Structural analysis and biological activities of BXL0124, a Gemini analog of Vitamin D==
		+	<StructureSection load='5lga' size='340' side='right' caption='[[5lga]], [[Resolution\|resolution]] 2.50Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5lga]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5LGA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5LGA FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6VH:(1~{R},3~{S},5~{Z})-5-[2-[(1~{R},3~{A}~{S},7~{A}~{R})-7~{A}-METHYL-1-[(6~{R})-1,1,1-TRIS(FLUORANYL)-10-METHYL-2,10-BIS(OXIDANYL)-2-(TRIFLUOROMETHYL)UNDECA-3,8-DIYN-6-YL]-2,3,3~{A},5,6,7-HEXAHYDRO-1~{H}-INDEN-4-YLIDENE]ETHYLIDENE]-4-METHYLIDENE-CYCLOHEXANE-1,3-DIOL'>6VH</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=5lga FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lga OCA], [http://pdbe.org/5lga PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5lga RCSB], [http://www.ebi.ac.uk/pdbsum/5lga PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5lga ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/VDRA_DANRE VDRA_DANRE]] Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Regulates transcription of hormone sensitive genes via its association with the WINAC complex, a chromatin-remodeling complex. Plays a central role in calcium homeostasis.<ref>PMID:17218092</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Gemini analogs of calcitriol, characterized by the extension of the C21-methyl group of calcitriol with a second chain, act as agonists of the vitamin D receptor (VDR). This second side chain of gemini is accommodated in a new cavity inside the VDR created by the structural rearrangement of the protein core. The resulting conformational change preserves the active state of the receptor and bestows gemini compounds with biological activities that exceed those of calcitriol. Of particular interest are gemini's anti-cancer properties, and in this study we demonstrate anti-proliferative and tumor-reducing abilities of BXL0124 and BXL0097, differing only by the presence or absence, respectively, of the methylene group on the A ring. BXL0124 acts as a more potent VDR agonist than its 19-nor counterpart by activating VDR-mediated transcription at lower concentrations. In a similar manner, BXL0124 is more active than BXL0097 in growth inhibition of breast cancer cells and reduction of tumor volume. Structural comparisons of BXL0097 and BXL0124, as their VDR complexes, explain the elevated activity of the latter.

-	~~Authors~~:	+	Structural analysis and biological activities of BXL0124, a gemini analog of vitamin D.,Belorusova AY, Suh N, Lee HJ, So JY, Maehr H, Rochel N J Steroid Biochem Mol Biol. 2016 Sep 17. pii: S0960-0760(16)30251-5. doi:, 10.1016/j.jsbmb.2016.09.015. PMID:27650654<ref>PMID:27650654</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
		+	<div class="pdbe-citations 5lga" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Belorusova, A Y]]
		+	[[Category: Rochel, N]]
		+	[[Category: Agonist]]
		+	[[Category: Gemini]]
		+	[[Category: Transcription]]
		+	[[Category: Vitamin d nuclear receptor]]

OCA at 02:46, 4 August 2016

2016-08-04T02:46:12Z

←Older revision		Revision as of 02:46, 4 August 2016
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 5lga is ON HOLD	+	The entry 5lga is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "5lga" [edit=sysop:move=sysop]

2016-07-14T10:06:18Z

Protected "5lga" [edit=sysop:move=sysop]

←Older revision

Revision as of 10:06, 14 July 2016

OCA: New page: '''Unreleased structure''' The entry 5lga is ON HOLD Authors: Description: Category: Unreleased Structures

2016-07-14T10:06:16Z

New page: '''Unreleased structure''' The entry 5lga is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 5lga is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]