4ql1 - Revision history

OCA at 17:33, 20 September 2023

2023-09-20T17:33:08Z

←Older revision		Revision as of 17:33, 20 September 2023
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	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4ql1]] 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=4QL1 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4QL1 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4ql1]] 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=4QL1 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4QL1 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=35Q:N-(4-(4-METHYLPIPERAZIN-1-YL)-3-(MORPHOLINOMETHYL)-[1,1-BIPHENYL]-3-YL)-6-OXO-4-(TRIFLUOROMETHYL)-1,6-DIHYDROPYRIDINE-3-CARBOXAMIDE'>35Q</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</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]] 1.5Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=35Q:N-(4-(4-METHYLPIPERAZIN-1-YL)-3-(MORPHOLINOMETHYL)-[1,1-BIPHENYL]-3-YL)-6-OXO-4-(TRIFLUOROMETHYL)-1,6-DIHYDROPYRIDINE-3-CARBOXAMIDE'>35Q</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [https://pdbe.org/4ql1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [https://www.ebi.ac.uk/pdbsum/4ql1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ql1 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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [https://pdbe.org/4ql1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [https://www.ebi.ac.uk/pdbsum/4ql1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ql1 ProSAT]</span></td></tr>
	</table>		</table>

OCA at 11:34, 15 February 2023

2023-02-15T11:34:17Z

←Older revision		Revision as of 11:34, 15 February 2023
Line 3:		Line 3:
	<StructureSection load='4ql1' size='340' side='right'caption='[[4ql1]], [[Resolution\|resolution]] 1.50Å' scene=''>		<StructureSection load='4ql1' size='340' side='right'caption='[[4ql1]], [[Resolution\|resolution]] 1.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4ql1]] is a 2 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=4QL1 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4QL1 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4ql1]] 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=4QL1 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4QL1 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=35Q:N-(4-(4-METHYLPIPERAZIN-1-YL)-3-(MORPHOLINOMETHYL)-[1,1-BIPHENYL]-3-YL)-6-OXO-4-(TRIFLUOROMETHYL)-1,6-DIHYDROPYRIDINE-3-CARBOXAMIDE'>35Q</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</scene>~~</td></tr>~~	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=35Q:N-(4-(4-METHYLPIPERAZIN-1-YL)-3-(MORPHOLINOMETHYL)-[1,1-BIPHENYL]-3-YL)-6-OXO-4-(TRIFLUOROMETHYL)-1,6-DIHYDROPYRIDINE-3-CARBOXAMIDE'>35Q</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</scene></td></tr>
-	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">WDR5, BIG3 ([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'>[https://proteopedia.org/fgij/fg.htm?mol=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [https://pdbe.org/4ql1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [https://www.ebi.ac.uk/pdbsum/4ql1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ql1 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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [~~http~~://pdbe.org/4ql1 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4ql1 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4ql1 ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/WDR5_HUMAN WDR5_HUMAN]] Contributes to histone modification. May position the N-terminus of histone H3 for efficient trimethylation at 'Lys-4'. As part of the MLL1/MLL complex it is involved in methylation and dimethylation at 'Lys-4' of histone H3. H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation. As part of the NSL complex it may be involved in acetylation of nucleosomal histone H4 on several lysine residues. May regulate osteoblasts differentiation.<ref>PMID:19556245</ref> <ref>PMID:19103755</ref> <ref>PMID:20018852</ref> <ref>PMID:16600877</ref> <ref>PMID:16829960</ref>	+	[https://www.uniprot.org/uniprot/WDR5_HUMAN WDR5_HUMAN] Contributes to histone modification. May position the N-terminus of histone H3 for efficient trimethylation at 'Lys-4'. As part of the MLL1/MLL complex it is involved in methylation and dimethylation at 'Lys-4' of histone H3. H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation. As part of the NSL complex it may be involved in acetylation of nucleosomal histone H4 on several lysine residues. May regulate osteoblasts differentiation.<ref>PMID:19556245</ref> <ref>PMID:19103755</ref> <ref>PMID:20018852</ref> <ref>PMID:16600877</ref> <ref>PMID:16829960</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 21:		Line 20:

	==See Also==		==See Also==
-	*[[WD ~~repeat~~-~~containing~~ protein\|WD ~~repeat~~-~~containing~~ protein]]	+	*[[WD-repeat protein 3D structures\|WD-repeat protein 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Al-Awar, R]]	+	[[Category: Al-Awar R]]
-	[[Category: Arrowsmith~~, C H~~]]	+	[[Category: Arrowsmith CH]]
-	[[Category: Barsyte, D]]	+	[[Category: Barsyte D]]
-	[[Category: Bountra, C]]	+	[[Category: Bountra C]]
-	[[Category: Brown~~, P J~~]]	+	[[Category: Brown PJ]]
-	[[Category: Dombrovski, L]]	+	[[Category: Dombrovski L]]
-	[[Category: Dong, A]]	+	[[Category: Dong A]]
-	[[Category: Edwards~~, A M~~]]	+	[[Category: Edwards AM]]
-	[[Category: Getlik, M]]	+	[[Category: Getlik M]]
-	[[Category: Kuznetsova, E]]	+	[[Category: Kuznetsova E]]
-	[[Category: Li, F]]	+	[[Category: Li F]]
-	[[Category: Marcellus, R]]	+	[[Category: Marcellus R]]
-	[[Category: Poda, G]]	+	[[Category: Poda G]]
-	~~[[Category: Structural genomic~~]]	+	[[Category: Schapira M]]
-	[[Category: Schapira, M]]	+	[[Category: Senisterra G]]
-	[[Category: Senisterra, G]]	+	[[Category: Smil D]]
-	[[Category: Smil, D]]	+	[[Category: Vedadi M]]
-	[[Category: Vedadi, M]]	+	[[Category: Walker JR]]
-	[[Category: Walker~~, J R~~]]	+	[[Category: Wu H]]
-	[[Category: Wu, H]]	+
-	~~[[Category: Oicr-9429 inhibitor]]~~	+
-	~~[[Category: Sgc]]~~	+
-	~~[[Category: Transcription-inhibitor complex]]~~	+
-	~~[[Category: Wd repeat domain 5]]~~	+
-	~~[[Category: Wdr5~~]]	+

OCA at 09:22, 24 April 2019

2019-04-24T09:22:42Z

←Older revision		Revision as of 09:22, 24 April 2019
Line 1:		Line 1:

	==Crystal structure of human WDR5 in complex with compound OICR-9429==		==Crystal structure of human WDR5 in complex with compound OICR-9429==
-	<StructureSection load='4ql1' size='340' side='right' caption='[[4ql1]], [[Resolution\|resolution]] 1.50Å' scene=''>	+	<StructureSection load='4ql1' size='340' side='right'caption='[[4ql1]], [[Resolution\|resolution]] 1.50Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4ql1]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4QL1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4QL1 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4ql1]] is a 2 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=4QL1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4QL1 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=35Q:N-(4-(4-METHYLPIPERAZIN-1-YL)-3-(MORPHOLINOMETHYL)-[1,1-BIPHENYL]-3-YL)-6-OXO-4-(TRIFLUOROMETHYL)-1,6-DIHYDROPYRIDINE-3-CARBOXAMIDE'>35Q</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=35Q:N-(4-(4-METHYLPIPERAZIN-1-YL)-3-(MORPHOLINOMETHYL)-[1,1-BIPHENYL]-3-YL)-6-OXO-4-(TRIFLUOROMETHYL)-1,6-DIHYDROPYRIDINE-3-CARBOXAMIDE'>35Q</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [http://pdbe.org/4ql1 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [http://www.ebi.ac.uk/pdbsum/4ql1 PDBsum]</span></td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">WDR5, BIG3 ([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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [http://pdbe.org/4ql1 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [http://www.ebi.ac.uk/pdbsum/4ql1 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4ql1 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 20:		Line 21:

	==See Also==		==See Also==
-	*[[WD-repeat protein 5\|WD-repeat protein 5]]	+	*[[WD repeat-containing protein\|WD repeat-containing protein]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Al-Awar, R]]		[[Category: Al-Awar, R]]
	[[Category: Arrowsmith, C H]]		[[Category: Arrowsmith, C H]]

OCA at 10:24, 26 February 2016

2016-02-26T10:24:03Z

←Older revision		Revision as of 10:24, 26 February 2016
Line 1:		Line 1:
		+
	==Crystal structure of human WDR5 in complex with compound OICR-9429==		==Crystal structure of human WDR5 in complex with compound OICR-9429==
	<StructureSection load='4ql1' size='340' side='right' caption='[[4ql1]], [[Resolution\|resolution]] 1.50Å' scene=''>		<StructureSection load='4ql1' size='340' side='right' caption='[[4ql1]], [[Resolution\|resolution]] 1.50Å' scene=''>
Line 4:		Line 5:
	<table><tr><td colspan='2'>[[4ql1]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4QL1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4QL1 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4ql1]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4QL1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4QL1 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=35Q:N-(4-(4-METHYLPIPERAZIN-1-YL)-3-(MORPHOLINOMETHYL)-[1,1-BIPHENYL]-3-YL)-6-OXO-4-(TRIFLUOROMETHYL)-1,6-DIHYDROPYRIDINE-3-CARBOXAMIDE'>35Q</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=35Q:N-(4-(4-METHYLPIPERAZIN-1-YL)-3-(MORPHOLINOMETHYL)-[1,1-BIPHENYL]-3-YL)-6-OXO-4-(TRIFLUOROMETHYL)-1,6-DIHYDROPYRIDINE-3-CARBOXAMIDE'>35Q</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [http://www.ebi.ac.uk/pdbsum/4ql1 PDBsum]</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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [http://pdbe.org/4ql1 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [http://www.ebi.ac.uk/pdbsum/4ql1 PDBsum]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 16:		Line 17:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
		+	<div class="pdbe-citations 4ql1" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[WD-repeat protein 5\|WD-repeat protein 5]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 08:32, 29 July 2015

2015-07-29T08:32:45Z

←Older revision		Revision as of 08:32, 29 July 2015
Line 8:		Line 8:
	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/WDR5_HUMAN WDR5_HUMAN]] Contributes to histone modification. May position the N-terminus of histone H3 for efficient trimethylation at 'Lys-4'. As part of the MLL1/MLL complex it is involved in methylation and dimethylation at 'Lys-4' of histone H3. H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation. As part of the NSL complex it may be involved in acetylation of nucleosomal histone H4 on several lysine residues. May regulate osteoblasts differentiation.<ref>PMID:19556245</ref> <ref>PMID:19103755</ref> <ref>PMID:20018852</ref> <ref>PMID:16600877</ref> <ref>PMID:16829960</ref>		[[http://www.uniprot.org/uniprot/WDR5_HUMAN WDR5_HUMAN]] Contributes to histone modification. May position the N-terminus of histone H3 for efficient trimethylation at 'Lys-4'. As part of the MLL1/MLL complex it is involved in methylation and dimethylation at 'Lys-4' of histone H3. H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation. As part of the NSL complex it may be involved in acetylation of nucleosomal histone H4 on several lysine residues. May regulate osteoblasts differentiation.<ref>PMID:19556245</ref> <ref>PMID:19103755</ref> <ref>PMID:20018852</ref> <ref>PMID:16600877</ref> <ref>PMID:16829960</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The CEBPA gene is mutated in 9% of patients with acute myeloid leukemia (AML). Selective expression of a short (30-kDa) CCAAT-enhancer binding protein-alpha (C/EBPalpha) translational isoform, termed p30, represents the most common type of CEBPA mutation in AML. The molecular mechanisms underlying p30-mediated transformation remain incompletely understood. We show that C/EBPalpha p30, but not the normal p42 isoform, preferentially interacts with Wdr5, a key component of SET/MLL (SET-domain/mixed-lineage leukemia) histone-methyltransferase complexes. Accordingly, p30-bound genomic regions were enriched for MLL-dependent H3K4me3 marks. The p30-dependent increase in self-renewal and inhibition of myeloid differentiation required Wdr5, as downregulation of the latter inhibited proliferation and restored differentiation in p30-dependent AML models. OICR-9429 is a new small-molecule antagonist of the Wdr5-MLL interaction. This compound selectively inhibited proliferation and induced differentiation in p30-expressing human AML cells. Our data reveal the mechanism of p30-dependent transformation and establish the essential p30 cofactor Wdr5 as a therapeutic target in CEBPA-mutant AML.
		+
		+	Pharmacological targeting of the Wdr5-MLL interaction in C/EBPalpha N-terminal leukemia.,Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G, Stukalov A, Huber KV, Schonegger A, Marcellus R, Bilban M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G Nat Chem Biol. 2015 Aug;11(8):571-8. doi: 10.1038/nchembio.1859. Epub 2015 Jul, 13. PMID:26167872<ref>PMID:26167872</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 06:39, 15 April 2015

2015-04-15T06:39:31Z

←Older revision		Revision as of 06:39, 15 April 2015
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4ql1]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4QL1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4QL1 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4ql1]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4QL1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4QL1 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=35Q:N-{4-(4-METHYLPIPERAZIN-1-YL)-3-[(~~TETRAHYDRO~~-2H-~~PYRAN-4-YLAMINO)METHYL~~]~~BIPHENYL~~-3-YL}-6-OXO-4-(TRIFLUOROMETHYL)-1,6-DIHYDROPYRIDINE-3-CARBOXAMIDE'>35Q</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=35Q:N-(4-(4-METHYLPIPERAZIN-1-YL)-3-(MORPHOLINOMETHYL)-[1,1-BIPHENYL]-3-YL)-6-OXO-4-(TRIFLUOROMETHYL)-1,6-DIHYDROPYRIDINE-3-CARBOXAMIDE'>35Q</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [http://www.ebi.ac.uk/pdbsum/4ql1 PDBsum]</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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [http://www.ebi.ac.uk/pdbsum/4ql1 PDBsum]</span></td></tr>
	</table>		</table>

OCA at 05:39, 25 December 2014

2014-12-25T05:39:00Z

←Older revision		Revision as of 05:39, 25 December 2014
Line 6:		Line 6:
	<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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [http://www.ebi.ac.uk/pdbsum/4ql1 PDBsum]</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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [http://www.ebi.ac.uk/pdbsum/4ql1 PDBsum]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/WDR5_HUMAN WDR5_HUMAN]] Contributes to histone modification. May position the N-terminus of histone H3 for efficient trimethylation at 'Lys-4'. As part of the MLL1/MLL complex it is involved in methylation and dimethylation at 'Lys-4' of histone H3. H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation. As part of the NSL complex it may be involved in acetylation of nucleosomal histone H4 on several lysine residues. May regulate osteoblasts differentiation.<ref>PMID:19556245</ref> <ref>PMID:19103755</ref> <ref>PMID:20018852</ref> <ref>PMID:16600877</ref> <ref>PMID:16829960</ref>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>

OCA at 12:58, 17 December 2014

2014-12-17T12:58:01Z

←Older revision		Revision as of 12:58, 17 December 2014
Line 1:		Line 1:
-	'''~~Unreleased structure~~'''	+	==Crystal structure of human WDR5 in complex with compound OICR-9429==
-		+	<StructureSection load='4ql1' size='340' side='right' caption='[[4ql1]], [[Resolution\|resolution]] 1.50Å' scene=''>
-	~~The entry~~ 4ql1 is ~~ON HOLD until Paper Publication~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[4ql1]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4QL1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4QL1 FirstGlance]. <br>
-	~~Authors~~: ~~Dong~~, A., ~~Dombrovski~~, L., ~~Walker~~, J.R.~~, Getlik, M~~.~~, Kuznetsova, E~~., ~~Smil, D~~.~~, Barsyte, D~~.~~, Li, F~~., ~~Poda, G~~.~~, Senisterra, G~~.~~, Marcellus, R~~., Al-Awar, R., Bountra, C., ~~Arrowsmith~~, ~~C.H.~~, Edwards, A.M., ~~Brown~~, ~~P.J.~~, Schapira, M., Vedadi, M., Wu, H~~., Structural Genomics Consortium (SGC)~~	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=35Q:N-{4-(4-METHYLPIPERAZIN-1-YL)-3-[(TETRAHYDRO-2H-PYRAN-4-YLAMINO)METHYL]BIPHENYL-3-YL}-6-OXO-4-(TRIFLUOROMETHYL)-1,6-DIHYDROPYRIDINE-3-CARBOXAMIDE'>35Q</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</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=4ql1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ql1 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ql1 RCSB], [http://www.ebi.ac.uk/pdbsum/4ql1 PDBsum]</span></td></tr>
-	~~Description~~:	+	</table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Al-Awar, R]]
		+	[[Category: Arrowsmith, C H]]
		+	[[Category: Barsyte, D]]
		+	[[Category: Bountra, C]]
		+	[[Category: Brown, P J]]
		+	[[Category: Dombrovski, L]]
		+	[[Category: Dong, A]]
		+	[[Category: Edwards, A M]]
		+	[[Category: Getlik, M]]
		+	[[Category: Kuznetsova, E]]
		+	[[Category: Li, F]]
		+	[[Category: Marcellus, R]]
		+	[[Category: Poda, G]]
		+	[[Category: Structural genomic]]
		+	[[Category: Schapira, M]]
		+	[[Category: Senisterra, G]]
		+	[[Category: Smil, D]]
		+	[[Category: Vedadi, M]]
		+	[[Category: Walker, J R]]
		+	[[Category: Wu, H]]
		+	[[Category: Oicr-9429 inhibitor]]
		+	[[Category: Sgc]]
		+	[[Category: Transcription-inhibitor complex]]
		+	[[Category: Wd repeat domain 5]]
		+	[[Category: Wdr5]]

OCA at 08:12, 24 September 2014

2014-09-24T08:12:04Z

←Older revision		Revision as of 08:12, 24 September 2014
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 4ql1 is ON HOLD	+	The entry 4ql1 is ON HOLD until Paper Publication

	Authors: Dong, A., Dombrovski, L., Walker, J.R., Getlik, M., Kuznetsova, E., Smil, D., Barsyte, D., Li, F., Poda, G., Senisterra, G., Marcellus, R., Al-Awar, R., Bountra, C., Arrowsmith, C.H., Edwards, A.M., Brown, P.J., Schapira, M., Vedadi, M., Wu, H., Structural Genomics Consortium (SGC)		Authors: Dong, A., Dombrovski, L., Walker, J.R., Getlik, M., Kuznetsova, E., Smil, D., Barsyte, D., Li, F., Poda, G., Senisterra, G., Marcellus, R., Al-Awar, R., Bountra, C., Arrowsmith, C.H., Edwards, A.M., Brown, P.J., Schapira, M., Vedadi, M., Wu, H., Structural Genomics Consortium (SGC)

	Description:		Description:

OCA at 01:08, 7 August 2014

2014-08-07T01:08:02Z

←Older revision		Revision as of 01:08, 7 August 2014
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 4ql1 is ON HOLD ~~until Paper Publication~~	+	The entry 4ql1 is ON HOLD

	Authors: Dong, A., Dombrovski, L., Walker, J.R., Getlik, M., Kuznetsova, E., Smil, D., Barsyte, D., Li, F., Poda, G., Senisterra, G., Marcellus, R., Al-Awar, R., Bountra, C., Arrowsmith, C.H., Edwards, A.M., Brown, P.J., Schapira, M., Vedadi, M., Wu, H., Structural Genomics Consortium (SGC)		Authors: Dong, A., Dombrovski, L., Walker, J.R., Getlik, M., Kuznetsova, E., Smil, D., Barsyte, D., Li, F., Poda, G., Senisterra, G., Marcellus, R., Al-Awar, R., Bountra, C., Arrowsmith, C.H., Edwards, A.M., Brown, P.J., Schapira, M., Vedadi, M., Wu, H., Structural Genomics Consortium (SGC)

	Description:		Description: