7o7b - Revision history

OCA at 11:17, 14 June 2023

2023-06-14T11:17:49Z

←Older revision		Revision as of 11:17, 14 June 2023
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	==Solution NMR Structure of the Neh1 Domain of Human Nuclear factor erythroid 2-related factor 2 (NRF2)==		==Solution NMR Structure of the Neh1 Domain of Human Nuclear factor erythroid 2-related factor 2 (NRF2)==
-	<StructureSection load='7o7b' size='340' side='right'caption='[[7o7b~~]], [[NMR_Ensembles_of_Models \| 20 NMR models~~]]' scene=''>	+	<StructureSection load='7o7b' size='340' side='right'caption='[[7o7b]]' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[7o7b]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7O7B OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7O7B FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[7o7b]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7O7B OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7O7B FirstGlance]. <br>
	</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=7o7b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7o7b OCA], [https://pdbe.org/7o7b PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7o7b RCSB], [https://www.ebi.ac.uk/pdbsum/7o7b PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7o7b ProSAT]</span></td></tr>		</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=7o7b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7o7b OCA], [https://pdbe.org/7o7b PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7o7b RCSB], [https://www.ebi.ac.uk/pdbsum/7o7b PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7o7b ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[https://www.uniprot.org/uniprot/NF2L2_HUMAN NF2L2_HUMAN]] Transcription activator that binds to antioxidant response (ARE) elements in the promoter regions of target genes. Important for the coordinated up-regulation of genes in response to oxidative stress. May be involved in the transcriptional activation of genes of the beta-globin cluster by mediating enhancer activity of hypersensitive site 2 of the beta-globin locus control region.<ref>PMID:11035812</ref>	+	[https://www.uniprot.org/uniprot/NF2L2_HUMAN NF2L2_HUMAN] Transcription activator that binds to antioxidant response (ARE) elements in the promoter regions of target genes. Important for the coordinated up-regulation of genes in response to oxidative stress. May be involved in the transcriptional activation of genes of the beta-globin cluster by mediating enhancer activity of hypersensitive site 2 of the beta-globin locus control region.<ref>PMID:11035812</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: Brueschweiler, S]]	+	[[Category: Brueschweiler S]]
-	~~[[Category: Antioxidant response]]~~	+
-	~~[[Category: Dna binding protein~~]]	+

OCA at 16:59, 15 December 2021

2021-12-15T16:59:49Z

←Older revision		Revision as of 16:59, 15 December 2021
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	==Solution NMR Structure of the Neh1 Domain of Human Nuclear factor erythroid 2-related factor 2 (NRF2)==		==Solution NMR Structure of the Neh1 Domain of Human Nuclear factor erythroid 2-related factor 2 (NRF2)==
-	<StructureSection load='7o7b' size='340' side='right'caption='[[7o7b]]' scene=''>	+	<StructureSection load='7o7b' size='340' side='right'caption='[[7o7b]], [[NMR_Ensembles_of_Models \| 20 NMR models]]' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>Full ~~crystallographic~~ information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7O7B OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7O7B FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[7o7b]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7O7B OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7O7B FirstGlance]. <br>
	</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=7o7b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7o7b OCA], [https://pdbe.org/7o7b PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7o7b RCSB], [https://www.ebi.ac.uk/pdbsum/7o7b PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7o7b ProSAT]</span></td></tr>		</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=7o7b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7o7b OCA], [https://pdbe.org/7o7b PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7o7b RCSB], [https://www.ebi.ac.uk/pdbsum/7o7b PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7o7b ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[https://www.uniprot.org/uniprot/NF2L2_HUMAN NF2L2_HUMAN]] Transcription activator that binds to antioxidant response (ARE) elements in the promoter regions of target genes. Important for the coordinated up-regulation of genes in response to oxidative stress. May be involved in the transcriptional activation of genes of the beta-globin cluster by mediating enhancer activity of hypersensitive site 2 of the beta-globin locus control region.<ref>PMID:11035812</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The NRF2 transcription factor is a key regulator in cellular oxidative stress response, and acts as a tumor suppressor. Aberrant activation of NRF2 has been implicated in promoting chemo-resistance, tumor growth, and metastasis by activating its downstream target genes. Hence, inhibition of NRF2 promises to be an attractive therapeutic strategy to suppress cell proliferation and enhance cell apoptosis in cancer. Direct targeting of NRF2 with small-molecules to discover protein-DNA inhibitors is challenging as it is a largely intrinsically disordered protein. To discover molecules that bind to NRF2 at the DNA binding interface, we performed an NMR-based fragment screen against its DNA-binding domain. We discovered several weakly binding fragment hits that bind to a region overlapping with the DNA binding site. Using SAR by catalogue we developed an initial structure-activity relationship for the most interesting initial hit series. By combining NMR chemical shift perturbations and data driven docking, binding poses which agreed with NMR information and the observed SAR were elucidated. The herein discovered NRF2 hits and proposed binding modes form the basis for future structure-based optimization campaigns on this important but to date 'undrugged' cancer driver.
		+
		+	A Step Towards NRF2-DNA Interaction Inhibitors by Fragment-Based NMR Methods.,Bruschweiler S, Fuchs JE, Bader G, McConnell DB, Konrat R, Mayer M ChemMedChem. 2021 Sep 15. doi: 10.1002/cmdc.202100458. PMID:34524728<ref>PMID:34524728</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 7o7b" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Brueschweiler S]]	+	[[Category: Brueschweiler, S]]
		+	[[Category: Antioxidant response]]
		+	[[Category: Dna binding protein]]

OCA at 08:51, 29 September 2021

2021-09-29T08:51:08Z

←Older revision		Revision as of 08:51, 29 September 2021
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-	'''Unreleased structure'''

-	~~The entry~~ 7o7b ~~is ON HOLD until Paper Publication~~	+	==Solution NMR Structure of the Neh1 Domain of Human Nuclear factor erythroid 2-related factor 2 (NRF2)==
-		+	<StructureSection load='7o7b' size='340' side='right'caption='[[7o7b]]' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7O7B OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7O7B FirstGlance]. <br>
-	~~Description~~:	+	</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=7o7b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7o7b OCA], [https://pdbe.org/7o7b PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7o7b RCSB], [https://www.ebi.ac.uk/pdbsum/7o7b PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7o7b ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	</table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Brueschweiler S]]

OCA at 08:20, 12 May 2021

2021-05-12T08:20:30Z

←Older revision		Revision as of 08:20, 12 May 2021
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 7o7b is ON HOLD	+	The entry 7o7b is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "7o7b" [edit=sysop:move=sysop]

2021-04-21T06:40:23Z

Protected "7o7b" [edit=sysop:move=sysop]

←Older revision

Revision as of 06:40, 21 April 2021

OCA: New page: '''Unreleased structure''' The entry 7o7b is ON HOLD Authors: Description: Category: Unreleased Structures

2021-04-21T06:40:21Z

New page: '''Unreleased structure''' The entry 7o7b is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 7o7b is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]