5kyj - Revision history

OCA at 11:01, 27 September 2023

OCA — Wed, 27 Sep 2023 11:01:44 GMT

←Older revision		Revision as of 11:01, 27 September 2023
Line 3:		Line 3:
	<StructureSection load='5kyj' size='340' side='right'caption='[[5kyj]], [[Resolution\|resolution]] 2.80Å' scene=''>		<StructureSection load='5kyj' size='340' side='right'caption='[[5kyj]], [[Resolution\|resolution]] 2.80Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5kyj]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5KYJ OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=5KYJ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5kyj]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5KYJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5KYJ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6Y8:(6~{R})-5-(5-FLUORANYL-2-METHOXY-PYRIMIDIN-4-YL)-2-(3-METHYLSULFONYLPHENYL)-6-PROPAN-2-YL-4,6-DIHYDROPYRROLO[3,4-C]PYRAZOLE'>6Y8</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]] 2.8Å</td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5i4v\|5i4v]], [[5kya\|5kya]]~~</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6Y8:(6~{R})-5-(5-FLUORANYL-2-METHOXY-PYRIMIDIN-4-YL)-2-(3-METHYLSULFONYLPHENYL)-6-PROPAN-2-YL-4,6-DIHYDROPYRROLO[3,4-C]PYRAZOLE'>6Y8</scene></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=5kyj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kyj OCA], [~~http~~://pdbe.org/5kyj PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5kyj RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5kyj PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5kyj 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=5kyj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kyj OCA], [https://pdbe.org/5kyj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5kyj RCSB], [https://www.ebi.ac.uk/pdbsum/5kyj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5kyj 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/RXRB_HUMAN RXRB_HUMAN]] Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5 (By similarity). Specifically binds 9-cis retinoic acid (9C-RA).	+	[https://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;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 27:		Line 27:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Chen, G]]	+	[[Category: Chen G]]
-	[[Category: McKeever~~, B M]]~~	+	[[Category: McKeever BM]]
-	~~[[Category: Chemical modulator]]~~	+
-	~~[[Category: Dna binding protein]]~~	+
-	~~[[Category: Liver x receptor]]~~	+
-	~~[[Category: Lxrbeta-lbd/rxrbeta-lbd heterodimer]]~~	+
-	~~[[Category: Nuclear receptor]]~~	+
-	~~[[Category: Retinoic acid x receptor~~]]	+

OCA at 06:37, 5 August 2020

OCA — Wed, 05 Aug 2020 06:37:30 GMT

←Older revision		Revision as of 06:37, 5 August 2020
Line 1:		Line 1:

	==Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core==		==Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core==
-	<StructureSection load='5kyj' size='340' side='right' caption='[[5kyj]], [[Resolution\|resolution]] 2.80Å' scene=''>	+	<StructureSection load='5kyj' size='340' side='right'caption='[[5kyj]], [[Resolution\|resolution]] 2.80Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5kyj]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5KYJ OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5KYJ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5kyj]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5KYJ OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5KYJ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6Y8:(6~{R})-5-(5-FLUORANYL-2-METHOXY-PYRIMIDIN-4-YL)-2-(3-METHYLSULFONYLPHENYL)-6-PROPAN-2-YL-4,6-DIHYDROPYRROLO[3,4-C]PYRAZOLE'>6Y8</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6Y8:(6~{R})-5-(5-FLUORANYL-2-METHOXY-PYRIMIDIN-4-YL)-2-(3-METHYLSULFONYLPHENYL)-6-PROPAN-2-YL-4,6-DIHYDROPYRROLO[3,4-C]PYRAZOLE'>6Y8</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5i4v\|5i4v]], [[5kya\|5kya]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5i4v\|5i4v]], [[5kya\|5kya]]</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=5kyj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kyj OCA], [http://pdbe.org/5kyj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5kyj RCSB], [http://www.ebi.ac.uk/pdbsum/5kyj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5kyj 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=5kyj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kyj OCA], [http://pdbe.org/5kyj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5kyj RCSB], [http://www.ebi.ac.uk/pdbsum/5kyj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5kyj ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 19:		Line 19:
	</div>		</div>
	<div class="pdbe-citations 5kyj" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 5kyj" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Liver X receptor\|Liver X receptor]]
		+	*[[Retinoid X receptor 3D structures\|Retinoid X receptor 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Chen, G]]		[[Category: Chen, G]]
	[[Category: McKeever, B M]]		[[Category: McKeever, B M]]

OCA at 13:57, 21 September 2016

OCA — Wed, 21 Sep 2016 13:57:58 GMT

←Older revision		Revision as of 13:57, 21 September 2016
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 5kyj is ~~ON HOLD until Paper~~ Publication	+	==Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core==
		+	<StructureSection load='5kyj' size='340' side='right' caption='[[5kyj]], [[Resolution\|resolution]] 2.80Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5kyj]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5KYJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5KYJ FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6Y8:(6~{R})-5-(5-FLUORANYL-2-METHOXY-PYRIMIDIN-4-YL)-2-(3-METHYLSULFONYLPHENYL)-6-PROPAN-2-YL-4,6-DIHYDROPYRROLO[3,4-C]PYRAZOLE'>6Y8</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5i4v\|5i4v]], [[5kya\|5kya]]</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=5kyj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kyj OCA], [http://pdbe.org/5kyj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5kyj RCSB], [http://www.ebi.ac.uk/pdbsum/5kyj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5kyj 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). [[http://www.uniprot.org/uniprot/RXRB_HUMAN RXRB_HUMAN]] Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5 (By similarity). Specifically binds 9-cis retinoic acid (9C-RA).
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Liver X receptor (LXR) agonists have been reported to lower brain amyloid beta (Abeta) and thus to have potential for the treatment of Alzheimer's disease. Structure and property based design led to the discovery of a series of orally bioavailable, brain penetrant LXR agonists. Oral administration of compound 18 to rats resulted in significant upregulation of the expression of the LXR target gene ABCA1 in brain tissue, but no significant effect on Abeta levels was detected.

-	~~Authors~~:	+	Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.,Tice CM, Noto PB, Fan KY, Zhao W, Lotesta SD, Dong C, Marcus AP, Zheng YJ, Chen G, Wu Z, Van Orden R, Zhou J, Bukhtiyarov Y, Zhao Y, Lipinski K, Howard L, Guo J, Kandpal G, Meng S, Hardy A, Krosky P, Gregg RE, Leftheris K, McKeever BM, Singh SB, Lala D, McGeehan GM, Zhuang L, Claremon DA Bioorg Med Chem Lett. 2016 Aug 29. pii: S0960-894X(16)30921-0. doi:, 10.1016/j.bmcl.2016.08.089. PMID:27599745<ref>PMID:27599745</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
		+	<div class="pdbe-citations 5kyj" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Chen, G]]
		+	[[Category: McKeever, B M]]
		+	[[Category: Chemical modulator]]
		+	[[Category: Dna binding protein]]
		+	[[Category: Liver x receptor]]
		+	[[Category: Lxrbeta-lbd/rxrbeta-lbd heterodimer]]
		+	[[Category: Nuclear receptor]]
		+	[[Category: Retinoic acid x receptor]]

OCA at 14:26, 9 September 2016

OCA — Fri, 09 Sep 2016 14:26:39 GMT

←Older revision		Revision as of 14:26, 9 September 2016
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

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

	Authors:		Authors:

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

OCA — Wed, 27 Jul 2016 13:32:34 GMT

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

←Older revision

Revision as of 13:32, 27 July 2016

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

OCA — Wed, 27 Jul 2016 13:32:33 GMT

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

New page

'''Unreleased structure'''

The entry 5kyj is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]