4zql - Revision history

OCA at 11:00, 10 January 2024

OCA — Wed, 10 Jan 2024 11:00:52 GMT

←Older revision		Revision as of 11:00, 10 January 2024
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	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4zql]] 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=4ZQL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4ZQL FirstGlance]. <br>		<table><tr><td colspan='2'>[[4zql]] 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=4ZQL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4ZQL FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=4QH:3,4-DIMETHOXY-N-[6-(4-METHOXYPHENOXY)-1,3-DIMETHYL-2-OXO-2,3-DIHYDRO-1H-BENZIMIDAZOL-5-YL]BENZENESULFONAMIDE'>4QH</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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]] 1.79Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=4QH:3,4-DIMETHOXY-N-[6-(4-METHOXYPHENOXY)-1,3-DIMETHYL-2-OXO-2,3-DIHYDRO-1H-BENZIMIDAZOL-5-YL]BENZENESULFONAMIDE'>4QH</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=4zql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zql OCA], [https://pdbe.org/4zql PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4zql RCSB], [https://www.ebi.ac.uk/pdbsum/4zql PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4zql 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=4zql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zql OCA], [https://pdbe.org/4zql PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4zql RCSB], [https://www.ebi.ac.uk/pdbsum/4zql PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4zql ProSAT]</span></td></tr>
	</table>		</table>

OCA at 07:37, 18 May 2023

OCA — Thu, 18 May 2023 07:37:58 GMT

←Older revision		Revision as of 07:37, 18 May 2023
Line 3:		Line 3:
	<StructureSection load='4zql' size='340' side='right'caption='[[4zql]], [[Resolution\|resolution]] 1.79Å' scene=''>		<StructureSection load='4zql' size='340' side='right'caption='[[4zql]], [[Resolution\|resolution]] 1.79Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4zql]] 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=4ZQL OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4ZQL FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4zql]] 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=4ZQL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4ZQL FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=4QH:3,4-DIMETHOXY-N-[6-(4-METHOXYPHENOXY)-1,3-DIMETHYL-2-OXO-2,3-DIHYDRO-1H-BENZIMIDAZOL-5-YL]BENZENESULFONAMIDE'>4QH</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>~~</td></tr>~~	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=4QH:3,4-DIMETHOXY-N-[6-(4-METHOXYPHENOXY)-1,3-DIMETHYL-2-OXO-2,3-DIHYDRO-1H-BENZIMIDAZOL-5-YL]BENZENESULFONAMIDE'>4QH</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">TRIM24, RNF82, TIF1, TIF1A ([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=4zql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zql OCA], [https://pdbe.org/4zql PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4zql RCSB], [https://www.ebi.ac.uk/pdbsum/4zql PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4zql 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=4zql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zql OCA], [~~http~~://pdbe.org/4zql PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4zql RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4zql PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4zql ProSAT]</span></td></tr>	+
	</table>		</table>
	== Disease ==		== Disease ==
-	[~~[http~~://www.uniprot.org/uniprot/TIF1A_HUMAN TIF1A_HUMAN]] Defects in TRIM24 are a cause of thyroid papillary carcinoma (TPC) [MIM:[~~http~~://omim.org/entry/188550 188550]]. TPC is a common tumor of the thyroid that typically arises as an irregular, solid or cystic mass from otherwise normal thyroid tissue. Papillary carcinomas are malignant neoplasm characterized by the formation of numerous, irregular, finger-like projections of fibrous stroma that is covered with a surface layer of neoplastic epithelial cells. Note=A chromosomal aberration involving TRIM24/TIF1 is found in thyroid papillary carcinomas. Translocation t(7;10)(q32;q11) with RET. The translocation generates the TRIM24/RET (PTC6) oncogene.	+	[https://www.uniprot.org/uniprot/TIF1A_HUMAN TIF1A_HUMAN] Defects in TRIM24 are a cause of thyroid papillary carcinoma (TPC) [MIM:[https://omim.org/entry/188550 188550]. TPC is a common tumor of the thyroid that typically arises as an irregular, solid or cystic mass from otherwise normal thyroid tissue. Papillary carcinomas are malignant neoplasm characterized by the formation of numerous, irregular, finger-like projections of fibrous stroma that is covered with a surface layer of neoplastic epithelial cells. Note=A chromosomal aberration involving TRIM24/TIF1 is found in thyroid papillary carcinomas. Translocation t(7;10)(q32;q11) with RET. The translocation generates the TRIM24/RET (PTC6) oncogene.
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/TIF1A_HUMAN TIF1A_HUMAN]] Transcriptional coactivator that interacts with numerous nuclear receptors and coactivators and modulates the transcription of target genes. Interacts with chromatin depending on histone H3 modifications, having the highest affinity for histone H3 that is both unmodified at 'Lys-4' (H3K4me0) and acetylated at 'Lys-23' (H3K23ac). Has E3 protein-ubiquitin ligase activity. Promotes ubiquitination and proteasomal degradation of p53/TP53. Plays a role in the regulation of cell proliferation and apoptosis, at least in part via its effects on p53/TP53 levels. Up-regulates ligand-dependent transcription activation by AR, GCR/NR3C1, thyroid hormone receptor (TR) and ESR1. Modulates transcription activation by retinoic acid (RA) receptors, including RARA. Plays a role in regulating retinoic acid-dependent proliferation of hepatocytes (By similarity).<ref>PMID:16322096</ref> <ref>PMID:19556538</ref> <ref>PMID:21164480</ref>	+	[https://www.uniprot.org/uniprot/TIF1A_HUMAN TIF1A_HUMAN] Transcriptional coactivator that interacts with numerous nuclear receptors and coactivators and modulates the transcription of target genes. Interacts with chromatin depending on histone H3 modifications, having the highest affinity for histone H3 that is both unmodified at 'Lys-4' (H3K4me0) and acetylated at 'Lys-23' (H3K23ac). Has E3 protein-ubiquitin ligase activity. Promotes ubiquitination and proteasomal degradation of p53/TP53. Plays a role in the regulation of cell proliferation and apoptosis, at least in part via its effects on p53/TP53 levels. Up-regulates ligand-dependent transcription activation by AR, GCR/NR3C1, thyroid hormone receptor (TR) and ESR1. Modulates transcription activation by retinoic acid (RA) receptors, including RARA. Plays a role in regulating retinoic acid-dependent proliferation of hepatocytes (By similarity).<ref>PMID:16322096</ref> <ref>PMID:19556538</ref> <ref>PMID:21164480</ref>
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Arrowsmith~~, C H~~]]	+	[[Category: Arrowsmith CH]]
-	[[Category: Bountra, C]]	+	[[Category: Bountra C]]
-	[[Category: Brennan~~, P E~~]]	+	[[Category: Brennan PE]]
-	[[Category: Clark~~, P G.K]]~~	+	[[Category: Clark PGK]]
-	~~[[Category: Delft, F von~~]]	+	[[Category: Dixon DJ]]
-	[[Category: Dixon~~, D J~~]]	+	[[Category: Edwards AM]]
-	[[Category: Edwards~~, A M~~]]	+	[[Category: Fedorov O]]
-	[[Category: Fedorov, O]]	+	[[Category: Knapp S]]
-	[[Category: Knapp, S]]	+	[[Category: Krojer T]]
-	[[Category: Krojer, T]]	+	[[Category: Nunez-Alonso G]]
-	[[Category: Nunez-Alonso, G]]	+	[[Category: Picaud S]]
-	[[Category: Picaud, S]]	+	[[Category: Tallant C]]
-	~~[[Category: Structural genomic~~]]	+	[[Category: Vieira LCC]]
-	[[Category: Tallant, C]]	+	[[Category: Von Delft F]]
-	[[Category: Vieira~~, L C.C~~]]	+
-	[[Category: ~~E3 protein-ubiquitin ligase activity]]~~	+
-	~~[[Category: Histone h3 modification]]~~	+
-	~~[[Category: Ligase]]~~	+
-	~~[[Category: Sgc]]~~	+
-	~~[[Category: Transcriptional coactivator~~]]	+

OCA at 08:02, 26 June 2019

OCA — Wed, 26 Jun 2019 08:02:34 GMT

←Older revision		Revision as of 08:02, 26 June 2019
Line 1:		Line 1:

	==Crystal structure of TRIM24 with 3,4-dimethoxy-N-(6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)benzenesulfonamide inhibitor==		==Crystal structure of TRIM24 with 3,4-dimethoxy-N-(6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)benzenesulfonamide inhibitor==
-	<StructureSection load='4zql' size='340' side='right' caption='[[4zql]], [[Resolution\|resolution]] 1.79Å' scene=''>	+	<StructureSection load='4zql' size='340' side='right'caption='[[4zql]], [[Resolution\|resolution]] 1.79Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4zql]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ZQL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ZQL FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4zql]] 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=4ZQL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ZQL FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=4QH:3,4-DIMETHOXY-N-[6-(4-METHOXYPHENOXY)-1,3-DIMETHYL-2-OXO-2,3-DIHYDRO-1H-BENZIMIDAZOL-5-YL]BENZENESULFONAMIDE'>4QH</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=4QH:3,4-DIMETHOXY-N-[6-(4-METHOXYPHENOXY)-1,3-DIMETHYL-2-OXO-2,3-DIHYDRO-1H-BENZIMIDAZOL-5-YL]BENZENESULFONAMIDE'>4QH</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">TRIM24, RNF82, TIF1, TIF1A ([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=4zql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zql OCA], [http://pdbe.org/4zql PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4zql RCSB], [http://www.ebi.ac.uk/pdbsum/4zql PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4zql 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=4zql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zql OCA], [http://pdbe.org/4zql PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4zql RCSB], [http://www.ebi.ac.uk/pdbsum/4zql PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4zql ProSAT]</span></td></tr>
	</table>		</table>
Line 15:		Line 16:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Arrowsmith, C H]]		[[Category: Arrowsmith, C H]]
	[[Category: Bountra, C]]		[[Category: Bountra, C]]

OCA at 17:06, 22 March 2017

OCA — Wed, 22 Mar 2017 17:06:35 GMT

←Older revision		Revision as of 17:06, 22 March 2017
Line 1:		Line 1:
		+
	==Crystal structure of TRIM24 with 3,4-dimethoxy-N-(6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)benzenesulfonamide inhibitor==		==Crystal structure of TRIM24 with 3,4-dimethoxy-N-(6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)benzenesulfonamide inhibitor==
	<StructureSection load='4zql' size='340' side='right' caption='[[4zql]], [[Resolution\|resolution]] 1.79Å' scene=''>		<StructureSection load='4zql' size='340' side='right' caption='[[4zql]], [[Resolution\|resolution]] 1.79Å' scene=''>
Line 4:		Line 5:
	<table><tr><td colspan='2'>[[4zql]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ZQL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ZQL FirstGlance]. <br>		<table><tr><td colspan='2'>[[4zql]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ZQL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ZQL FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=4QH:3,4-DIMETHOXY-N-[6-(4-METHOXYPHENOXY)-1,3-DIMETHYL-2-OXO-2,3-DIHYDRO-1H-BENZIMIDAZOL-5-YL]BENZENESULFONAMIDE'>4QH</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=4QH:3,4-DIMETHOXY-N-[6-(4-METHOXYPHENOXY)-1,3-DIMETHYL-2-OXO-2,3-DIHYDRO-1H-BENZIMIDAZOL-5-YL]BENZENESULFONAMIDE'>4QH</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=4zql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zql OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4zql RCSB], [http://www.ebi.ac.uk/pdbsum/4zql 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=4zql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zql OCA], [http://pdbe.org/4zql PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4zql RCSB], [http://www.ebi.ac.uk/pdbsum/4zql PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4zql ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==

OCA at 15:33, 17 June 2015

OCA — Wed, 17 Jun 2015 15:33:03 GMT

←Older revision		Revision as of 15:33, 17 June 2015
Line 1:		Line 1:
-	'''~~Unreleased structure~~'''	+	==Crystal structure of TRIM24 with 3,4-dimethoxy-N-(6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)benzenesulfonamide inhibitor==
-		+	<StructureSection load='4zql' size='340' side='right' caption='[[4zql]], [[Resolution\|resolution]] 1.79Å' scene=''>
-	~~The entry~~ 4zql is ~~ON HOLD~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[4zql]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ZQL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ZQL FirstGlance]. <br>
-	~~Authors~~: ~~Tallant~~, C., ~~Structural Genomics Consortium~~ (~~SGC~~), ~~Clark~~, ~~P.G.K.~~, ~~Vieira~~, L.C.C.~~, Krojer, T~~., ~~Nunez~~-~~Alonso~~, G.~~, Picaud, S~~.~~, Fedorov, O~~., ~~Dixon, D~~.J.~~, von Delft, F~~.~~, Arrowsmith, C~~.H.~~, Edwards, A~~.M., ~~Bountra, C~~., ~~Brennan~~, P.E.~~, Knapp, S~~.	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1PE:PENTAETHYLENE+GLYCOL'>1PE</scene>, <scene name='pdbligand=4QH:3,4-DIMETHOXY-N-[6-(4-METHOXYPHENOXY)-1,3-DIMETHYL-2-OXO-2,3-DIHYDRO-1H-BENZIMIDAZOL-5-YL]BENZENESULFONAMIDE'>4QH</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=4zql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4zql OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4zql RCSB], [http://www.ebi.ac.uk/pdbsum/4zql PDBsum]</span></td></tr>
-	~~Description~~: ~~Crystal structure~~ of ~~TRIM24~~ with 3,~~4-dimethoxy-N~~-(6-(~~4-methoxyphenoxy~~)-1,3-~~dimethyl~~-~~2-oxo-2~~,3-~~dihydro-1H-benzo~~[d]~~imidazol-5-yl)benzenesulfonamide inhibitor~~	+	</table>
-	[[Category: ~~Unreleased Structures~~]]	+	== Disease ==
-	[[Category: ~~Nunez-Alonso~~, G]]	+	[[http://www.uniprot.org/uniprot/TIF1A_HUMAN TIF1A_HUMAN]] Defects in TRIM24 are a cause of thyroid papillary carcinoma (TPC) [MIM:[http://omim.org/entry/188550 188550]]. TPC is a common tumor of the thyroid that typically arises as an irregular, solid or cystic mass from otherwise normal thyroid tissue. Papillary carcinomas are malignant neoplasm characterized by the formation of numerous, irregular, finger-like projections of fibrous stroma that is covered with a surface layer of neoplastic epithelial cells. Note=A chromosomal aberration involving TRIM24/TIF1 is found in thyroid papillary carcinomas. Translocation t(7;10)(q32;q11) with RET. The translocation generates the TRIM24/RET (PTC6) oncogene.
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/TIF1A_HUMAN TIF1A_HUMAN]] Transcriptional coactivator that interacts with numerous nuclear receptors and coactivators and modulates the transcription of target genes. Interacts with chromatin depending on histone H3 modifications, having the highest affinity for histone H3 that is both unmodified at 'Lys-4' (H3K4me0) and acetylated at 'Lys-23' (H3K23ac). Has E3 protein-ubiquitin ligase activity. Promotes ubiquitination and proteasomal degradation of p53/TP53. Plays a role in the regulation of cell proliferation and apoptosis, at least in part via its effects on p53/TP53 levels. Up-regulates ligand-dependent transcription activation by AR, GCR/NR3C1, thyroid hormone receptor (TR) and ESR1. Modulates transcription activation by retinoic acid (RA) receptors, including RARA. Plays a role in regulating retinoic acid-dependent proliferation of hepatocytes (By similarity).<ref>PMID:16322096</ref> <ref>PMID:19556538</ref> <ref>PMID:21164480</ref>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Arrowsmith, C H]]
		+	[[Category: Bountra, C]]
		+	[[Category: Brennan, P E]]
		+	[[Category: Clark, P G.K]]
		+	[[Category: Delft, F von]]
		+	[[Category: Dixon, D J]]
		+	[[Category: Edwards, A M]]
	[[Category: Fedorov, O]]		[[Category: Fedorov, O]]
-	[[Category: Vieira, L.C.C]]
-	[[Category: Picaud, S]]
	[[Category: Knapp, S]]		[[Category: Knapp, S]]
	[[Category: Krojer, T]]		[[Category: Krojer, T]]
-	[[Category: ~~Structural Genomics Consortium (Sgc), Clark~~, P.G.K]]	+	[[Category: Nunez-Alonso, G]]
-	[[Category: ~~Bountra~~, C]]	+	[[Category: Picaud, S]]
-	[[Category: ~~Arrowsmith, C.H]]~~	+	[[Category: Structural genomic]]
-	~~[[Category: Von Delft, F]]~~	+
-	~~[[Category: Edwards, A.M]]~~	+
-	~~[[Category: Dixon, D.J]]~~	+
-	~~[[Category: Brennan, P.E~~]]	+
	[[Category: Tallant, C]]		[[Category: Tallant, C]]
		+	[[Category: Vieira, L C.C]]
		+	[[Category: E3 protein-ubiquitin ligase activity]]
		+	[[Category: Histone h3 modification]]
		+	[[Category: Ligase]]
		+	[[Category: Sgc]]
		+	[[Category: Transcriptional coactivator]]

OCA: Protected "4zql" [edit=sysop:move=sysop]

OCA — Wed, 20 May 2015 11:01:05 GMT

Protected "4zql" [edit=sysop:move=sysop]

←Older revision

Revision as of 11:01, 20 May 2015

OCA: New page: '''Unreleased structure''' The entry 4zql is ON HOLD Authors: Tallant, C., Structural Genomics Consortium (SGC), Clark, P.G.K., Vieira, L.C.C., Krojer, T., Nunez-Alonso, G., Picaud, S.,...

OCA — Wed, 20 May 2015 11:01:04 GMT

New page: '''Unreleased structure''' The entry 4zql is ON HOLD Authors: Tallant, C., Structural Genomics Consortium (SGC), Clark, P.G.K., Vieira, L.C.C., Krojer, T., Nunez-Alonso, G., Picaud, S.,...

New page

'''Unreleased structure'''

The entry 4zql is ON HOLD

Authors: Tallant, C., Structural Genomics Consortium (SGC), Clark, P.G.K., Vieira, L.C.C., Krojer, T., Nunez-Alonso, G., Picaud, S., Fedorov, O., Dixon, D.J., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bountra, C., Brennan, P.E., Knapp, S.

Description: Crystal structure of TRIM24 with 3,4-dimethoxy-N-(6-(4-methoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)benzenesulfonamide inhibitor
[[Category: Unreleased Structures]]
[[Category: Nunez-Alonso, G]]
[[Category: Fedorov, O]]
[[Category: Vieira, L.C.C]]
[[Category: Picaud, S]]
[[Category: Knapp, S]]
[[Category: Krojer, T]]
[[Category: Structural Genomics Consortium (Sgc), Clark, P.G.K]]
[[Category: Bountra, C]]
[[Category: Arrowsmith, C.H]]
[[Category: Von Delft, F]]
[[Category: Edwards, A.M]]
[[Category: Dixon, D.J]]
[[Category: Brennan, P.E]]
[[Category: Tallant, C]]