5nqr - Revision history

OCA at 12:02, 22 November 2023

OCA — Wed, 22 Nov 2023 12:02:42 GMT

←Older revision		Revision as of 12:02, 22 November 2023
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	<StructureSection load='5nqr' size='340' side='right'caption='[[5nqr]], [[Resolution\|resolution]] 2.20Å' scene=''>		<StructureSection load='5nqr' size='340' side='right'caption='[[5nqr]], [[Resolution\|resolution]] 2.20Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5nqr]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5NQR OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=5NQR FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5nqr]] is a 2 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=5NQR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5NQR FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=958:8-(dimethylamino)-1,3-dimethyl-7-[[5-(3-methylphenyl)-1,3,4-oxadiazol-2-yl]methyl]purine-2,6-dione'>958</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]] 2.2Å</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=5nqr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5nqr OCA], [~~http~~://pdbe.org/5nqr PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5nqr RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5nqr PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5nqr ProSAT]</span></td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=958:8-(dimethylamino)-1,3-dimethyl-7-[[5-(3-methylphenyl)-1,3,4-oxadiazol-2-yl]methyl]purine-2,6-dione'>958</scene></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=5nqr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5nqr OCA], [https://pdbe.org/5nqr PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5nqr RCSB], [https://www.ebi.ac.uk/pdbsum/5nqr PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5nqr ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/NUDT5_HUMAN NUDT5_HUMAN]] Hydrolyzes with similar activities ADP-ribose ADP-mannose, ADP-glucose, 8-oxo-GDP and 8-oxo-dGDP. Can also hydrolyze other nucleotide sugars with low activity.<ref>PMID:17052728</ref>	+	[https://www.uniprot.org/uniprot/NUDT5_HUMAN NUDT5_HUMAN] Hydrolyzes with similar activities ADP-ribose ADP-mannose, ADP-glucose, 8-oxo-GDP and 8-oxo-dGDP. Can also hydrolyze other nucleotide sugars with low activity.<ref>PMID:17052728</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Carter, M]]	+	[[Category: Carter M]]
-	[[Category: Stenmark, P]]	+	[[Category: Stenmark P]]
-	~~[[Category: Hydrolase]]~~	+
-	~~[[Category: Inhibitor]]~~	+
-	~~[[Category: Nudix~~]]	+

OCA at 12:10, 26 August 2020

OCA — Wed, 26 Aug 2020 12:10:34 GMT

←Older revision		Revision as of 12:10, 26 August 2020
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	==Potent inhibitors of NUDT5 silence hormone signaling in breast cancer==		==Potent inhibitors of NUDT5 silence hormone signaling in breast cancer==
-	<StructureSection load='5nqr' size='340' side='right' caption='[[5nqr]], [[Resolution\|resolution]] 2.20Å' scene=''>	+	<StructureSection load='5nqr' size='340' side='right'caption='[[5nqr]], [[Resolution\|resolution]] 2.20Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5nqr]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5NQR OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5NQR FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5nqr]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5NQR OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5NQR FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=958:8-(dimethylamino)-1,3-dimethyl-7-[[5-(3-methylphenyl)-1,3,4-oxadiazol-2-yl]methyl]purine-2,6-dione'>958</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=958:8-(dimethylamino)-1,3-dimethyl-7-[[5-(3-methylphenyl)-1,3,4-oxadiazol-2-yl]methyl]purine-2,6-dione'>958</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=5nqr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5nqr OCA], [http://pdbe.org/5nqr PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5nqr RCSB], [http://www.ebi.ac.uk/pdbsum/5nqr PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5nqr 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=5nqr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5nqr OCA], [http://pdbe.org/5nqr PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5nqr RCSB], [http://www.ebi.ac.uk/pdbsum/5nqr PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5nqr ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Carter, M]]		[[Category: Carter, M]]
	[[Category: Stenmark, P]]		[[Category: Stenmark, P]]

OCA at 05:49, 31 January 2018

OCA — Wed, 31 Jan 2018 05:49:47 GMT

←Older revision		Revision as of 05:49, 31 January 2018
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-	'''Unreleased structure'''

-	~~The entry~~ 5nqr is ~~ON HOLD~~ ~~until Paper~~ Publication	+	==Potent inhibitors of NUDT5 silence hormone signaling in breast cancer==
		+	<StructureSection load='5nqr' size='340' side='right' caption='[[5nqr]], [[Resolution\|resolution]] 2.20Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5nqr]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5NQR OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5NQR FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=958:8-(dimethylamino)-1,3-dimethyl-7-[[5-(3-methylphenyl)-1,3,4-oxadiazol-2-yl]methyl]purine-2,6-dione'>958</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=5nqr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5nqr OCA], [http://pdbe.org/5nqr PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5nqr RCSB], [http://www.ebi.ac.uk/pdbsum/5nqr PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5nqr ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/NUDT5_HUMAN NUDT5_HUMAN]] Hydrolyzes with similar activities ADP-ribose ADP-mannose, ADP-glucose, 8-oxo-GDP and 8-oxo-dGDP. Can also hydrolyze other nucleotide sugars with low activity.<ref>PMID:17052728</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	With a diverse network of substrates, NUDIX hydrolases have emerged as a key family of nucleotide-metabolizing enzymes. NUDT5 (also called NUDIX5) has been implicated in ADP-ribose and 8-oxo-guanine metabolism and was recently identified as a rheostat of hormone-dependent gene regulation and proliferation in breast cancer cells. Here, we further elucidate the physiological relevance of known NUDT5 substrates and underscore the biological requirement for NUDT5 in gene regulation and proliferation of breast cancer cells. We confirm the involvement of NUDT5 in ADP-ribose metabolism and dissociate a relationship to oxidized nucleotide sanitation. Furthermore, we identify potent NUDT5 inhibitors, which are optimized to promote maximal NUDT5 cellular target engagement by CETSA. Lead compound, TH5427, blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells. We herein present TH5427 as a promising, targeted inhibitor that can be used to further study NUDT5 activity and ADP-ribose metabolism.

-	~~Authors~~:	+	Targeted NUDT5 inhibitors block hormone signaling in breast cancer cells.,Page BDG, Valerie NCK, Wright RHG, Wallner O, Isaksson R, Carter M, Rudd SG, Loseva O, Jemth AS, Almlof I, Font-Mateu J, Llona-Minguez S, Baranczewski P, Jeppsson F, Homan E, Almqvist H, Axelsson H, Regmi S, Gustavsson AL, Lundback T, Scobie M, Stromberg K, Stenmark P, Beato M, Helleday T Nat Commun. 2018 Jan 17;9(1):250. doi: 10.1038/s41467-017-02293-7. PMID:29343827<ref>PMID:29343827</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
		+	<div class="pdbe-citations 5nqr" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Carter, M]]
		+	[[Category: Stenmark, P]]
		+	[[Category: Hydrolase]]
		+	[[Category: Inhibitor]]
		+	[[Category: Nudix]]

OCA at 09:35, 4 May 2017

OCA — Thu, 04 May 2017 09:35:40 GMT

←Older revision		Revision as of 09:35, 4 May 2017
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

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

	Authors:		Authors:

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

OCA — Thu, 27 Apr 2017 10:48:40 GMT

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

←Older revision

Revision as of 10:48, 27 April 2017

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

OCA — Thu, 27 Apr 2017 10:48:39 GMT

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

New page

'''Unreleased structure'''

The entry 5nqr is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]