6s4t - Revision history

OCA at 18:46, 11 December 2019

OCA — Wed, 11 Dec 2019 18:46:31 GMT

←Older revision		Revision as of 18:46, 11 December 2019
Line 3:		Line 3:
	<StructureSection load='6s4t' size='340' side='right'caption='[[6s4t]], [[Resolution\|resolution]] 2.00Å' scene=''>		<StructureSection load='6s4t' size='340' side='right'caption='[[6s4t]], [[Resolution\|resolution]] 2.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6s4t]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6S4T OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6S4T FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6s4t]] is a 1 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=6S4T OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6S4T FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=KVB:2-[4-[[3-[3-(phenylmethyl)-8-(trifluoromethyl)quinolin-4-yl]phenoxy]methyl]phenyl]ethanoic+acid'>KVB</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=KVB:2-[4-[[3-[3-(phenylmethyl)-8-(trifluoromethyl)quinolin-4-yl]phenoxy]methyl]phenyl]ethanoic+acid'>KVB</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">NR1H2, LXRB, NER, UNR ([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=6s4t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6s4t OCA], [http://pdbe.org/6s4t PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6s4t RCSB], [http://www.ebi.ac.uk/pdbsum/6s4t PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6s4t 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=6s4t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6s4t OCA], [http://pdbe.org/6s4t PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6s4t RCSB], [http://www.ebi.ac.uk/pdbsum/6s4t PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6s4t ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/NR1H2_HUMAN NR1H2_HUMAN]] Orphan receptor. Binds preferentially to double-stranded oligonucleotide direct repeats having the consensus half-site sequence 5'-AGGTCA-3' and 4-nt spacing (DR-4). Regulates cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8 (By similarity).		[[http://www.uniprot.org/uniprot/NR1H2_HUMAN NR1H2_HUMAN]] Orphan receptor. Binds preferentially to double-stranded oligonucleotide direct repeats having the consensus half-site sequence 5'-AGGTCA-3' and 4-nt spacing (DR-4). Regulates cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8 (By similarity).
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Liver X receptors (LXRs) are attractive drug targets for cardiovascular disease treatment due to their role in regulating cholesterol homeostasis and immunity. The anti-atherogenic properties of LXRs have prompted development of synthetic ligands, but these cause major adverse effects-such as increased lipogenesis-which are challenging to dissect from their beneficial activities. Here we show that LXR compounds displaying diverse functional responses in animal models induce distinct receptor conformations. Combination of hydrogen/deuterium exchange mass spectrometry and multivariate analysis allowed identification of LXR regions differentially correlating with anti-atherogenic and lipogenic activities of ligands. We show that lipogenic compounds stabilize active states of LXRalpha and LXRbeta while the anti-atherogenic expression of the cholesterol transporter ABCA1 is associated with the ligand-induced stabilization of LXRalpha helix 3. Our data indicates that avoiding ligand interaction with the activation helix 12 while engaging helix 3 may provide directions for development of ligands with improved therapeutic profiles.
		+
		+	Structural analysis identifies an escape route from the adverse lipogenic effects of liver X receptor ligands.,Belorusova AY, Evertsson E, Hovdal D, Sandmark J, Bratt E, Maxvall I, Schulman IG, Akerblad P, Lindstedt EL Commun Biol. 2019 Nov 22;2:431. doi: 10.1038/s42003-019-0675-0. eCollection 2019. PMID:31799433<ref>PMID:31799433</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 6s4t" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Jansson, A]]		[[Category: Jansson, A]]

OCA at 06:57, 27 November 2019

OCA — Wed, 27 Nov 2019 06:57:54 GMT

←Older revision		Revision as of 06:57, 27 November 2019
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 6s4t is ~~ON HOLD~~	+	==LXRbeta ligand binding domain in comlpex with small molecule inhibitors==
-		+	<StructureSection load='6s4t' size='340' side='right'caption='[[6s4t]], [[Resolution\|resolution]] 2.00Å' scene=''>
-	~~Authors~~: ~~Sandmark~~, J., ~~Jansson~~, A.	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[6s4t]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6S4T OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6S4T FirstGlance]. <br>
-	~~Description~~: ~~LXRbeta ligand binding domain in comlpex with small molecule inhibitors~~	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=KVB:2-[4-[[3-[3-(phenylmethyl)-8-(trifluoromethyl)quinolin-4-yl]phenoxy]methyl]phenyl]ethanoic+acid'>KVB</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=6s4t FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6s4t OCA], [http://pdbe.org/6s4t PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6s4t RCSB], [http://www.ebi.ac.uk/pdbsum/6s4t PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6s4t ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/NR1H2_HUMAN NR1H2_HUMAN]] Orphan receptor. Binds preferentially to double-stranded oligonucleotide direct repeats having the consensus half-site sequence 5'-AGGTCA-3' and 4-nt spacing (DR-4). Regulates cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8 (By similarity).
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Jansson, A]]		[[Category: Jansson, A]]
	[[Category: Sandmark, J]]		[[Category: Sandmark, J]]
		+	[[Category: Liver x receptor beta lxrb lxr beta nuclear hormone receptor receptor ligand binding domain]]
		+	[[Category: Nuclear protein]]

OCA: Protected "6s4t" [edit=sysop:move=sysop]

OCA — Wed, 10 Jul 2019 04:23:40 GMT

Protected "6s4t" [edit=sysop:move=sysop]

←Older revision

Revision as of 04:23, 10 July 2019

OCA: New page: '''Unreleased structure''' The entry 6s4t is ON HOLD Authors: Sandmark, J., Jansson, A. Description: LXRbeta ligand binding domain in comlpex with small molecule inhibitors [[Category:...

OCA — Wed, 10 Jul 2019 04:23:39 GMT

New page: '''Unreleased structure''' The entry 6s4t is ON HOLD Authors: Sandmark, J., Jansson, A. Description: LXRbeta ligand binding domain in comlpex with small molecule inhibitors [[Category:...

New page

'''Unreleased structure'''

The entry 6s4t is ON HOLD

Authors: Sandmark, J., Jansson, A.

Description: LXRbeta ligand binding domain in comlpex with small molecule inhibitors
[[Category: Unreleased Structures]]
[[Category: Jansson, A]]
[[Category: Sandmark, J]]