OCA at 07:53, 18 December 2019

OCA — Wed, 18 Dec 2019 07:53:41 GMT

←Older revision		Revision as of 07:53, 18 December 2019
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 6s5k is ~~ON HOLD~~	+	==LXRbeta ligand binding domain in complex with small molecule inhibitors==
		+	<StructureSection load='6s5k' size='340' side='right'caption='[[6s5k]], [[Resolution\|resolution]] 1.60Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[6s5k]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6S5K OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6S5K FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=KWE:3-(4-phenylbutylamino)-1,4-bis(phenylmethyl)pyrrole-2,5-dione'>KWE</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=6s5k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6s5k OCA], [http://pdbe.org/6s5k PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6s5k RCSB], [http://www.ebi.ac.uk/pdbsum/6s5k PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6s5k 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).
		+	<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.

-	~~Authors: Petersen~~, J.	+	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>

-	~~Description~~: ~~LXRbeta ligand binding domain in complex with small molecule inhibitors~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased~~ Structures]]	+	</div>
		+	<div class="pdbe-citations 6s5k" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Petersen, J]]		[[Category: Petersen, J]]
		+	[[Category: Liver x receptor beta]]
		+	[[Category: Lxr beta]]
		+	[[Category: Lxrb]]
		+	[[Category: Nuclear hormone receptor]]
		+	[[Category: Nuclear protein]]
		+	[[Category: Receptor ligand binding domain]]

OCA at 04:22, 16 October 2019

OCA — Wed, 16 Oct 2019 04:22:22 GMT

←Older revision		Revision as of 04:22, 16 October 2019
Line 5:		Line 5:
	Authors: Petersen, J.		Authors: Petersen, J.

-	Description: LXRbeta ligand binding domain in ~~comlpex~~ with small molecule inhibitors	+	Description: LXRbeta ligand binding domain in complex with small molecule inhibitors
	[[Category: Unreleased Structures]]		[[Category: Unreleased Structures]]
	[[Category: Petersen, J]]		[[Category: Petersen, J]]

OCA: Protected "6s5k" [edit=sysop:move=sysop]

OCA — Wed, 10 Jul 2019 04:25:59 GMT

Protected "6s5k" [edit=sysop:move=sysop]

←Older revision

Revision as of 04:25, 10 July 2019

OCA: New page: '''Unreleased structure''' The entry 6s5k is ON HOLD Authors: Petersen, J. Description: LXRbeta ligand binding domain in comlpex with small molecule inhibitors [[Category: Unreleased S...

OCA — Wed, 10 Jul 2019 04:25:58 GMT

New page: '''Unreleased structure''' The entry 6s5k is ON HOLD Authors: Petersen, J. Description: LXRbeta ligand binding domain in comlpex with small molecule inhibitors [[Category: Unreleased S...

New page

'''Unreleased structure'''

The entry 6s5k is ON HOLD

Authors: Petersen, J.

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

6s5k - Revision history

OCA at 07:53, 18 December 2019

OCA at 04:22, 16 October 2019

OCA: Protected "6s5k" [edit=sysop:move=sysop]

OCA: New page: '''Unreleased structure''' The entry 6s5k is ON HOLD Authors: Petersen, J. Description: LXRbeta ligand binding domain in comlpex with small molecule inhibitors [[Category: Unreleased S...