OCA at 07:12, 2 September 2020

2020-09-02T07:12:55Z

←Older revision		Revision as of 07:12, 2 September 2020
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	==C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-acetamido-3-(benzyloxy)benzamide==		==C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-acetamido-3-(benzyloxy)benzamide==
-	<StructureSection load='6z7f' size='340' side='right'caption='[[6z7f]]' scene=''>	+	<StructureSection load='6z7f' size='340' side='right'caption='[[6z7f]], [[Resolution\|resolution]] 1.60Å' 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=6Z7F OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6Z7F FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6z7f]] is a 1 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=6Z7F OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6Z7F FirstGlance]. <br>
-	</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=6z7f FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6z7f OCA], [http://pdbe.org/6z7f PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6z7f RCSB], [http://www.ebi.ac.uk/pdbsum/6z7f PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6z7f ProSAT]</span></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene>, <scene name='pdbligand=QB5:N-(2-(1H-imidazol-4-yl)ethyl)-4-acetamido-3-(benzyloxy)benzamide'>QB5</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">BRD2, KIAA9001, RING3 ([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://proteopedia.org/fgij/fg.htm?mol=6z7f FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6z7f OCA], [http://pdbe.org/6z7f PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6z7f RCSB], [http://www.ebi.ac.uk/pdbsum/6z7f PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6z7f ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/BRD2_HUMAN BRD2_HUMAN]] May play a role in spermatogenesis or folliculogenesis (By similarity). Binds hyperacetylated chromatin and plays a role in the regulation of transcription, probably by chromatin remodeling. Regulates transcription of the CCND1 gene. Plays a role in nucleosome assembly.<ref>PMID:18406326</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Pan-BET inhibitors interact equipotently with the eight bromodomains of the BET family of proteins and have shown profound efficacy in a number of in vitro phenotypic assays and in vivo pre-clinical models in inflammation or oncology. A number of these inhibitors have progressed to the clinic where pharmacology-driven adverse events have been reported. To better understand the contribution of each domain to their efficacy and to improve from their safety profile, selective inhibitors are required. This article discloses the profile of GSK046, also known as iBET-BD2, a highly selective inhibitor of the second bromodomains of the BET proteins that has undergone extensive pre-clinical in vitro and in vivo characterisation.
		+
		+	The Design and Synthesis of a Highly Selective and In Vivo Capable Inhibitor of the Second Bromodomain (BD2) of the Bromodomain and Extra Terminal Domain (BET) Family of Proteins.,Preston A, Atkinson SJ, Bamborough P, Chung CW, Craggs PD, Gordon LJ, Grandi P, Gray J, Jones EJ, Lindon M, Michon AM, Mitchell DJ, Prinjha RK, Rianjongdee F, Rioja I, Seal J, Taylor S, Wall ID, Watson RJ, Woolven JM, Demont EH J Med Chem. 2020 Jul 21. doi: 10.1021/acs.jmedchem.0c00605. PMID:32691591<ref>PMID:32691591</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 6z7f" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Chung C]]	+	[[Category: Chung, C]]
		+	[[Category: Antagonist]]
		+	[[Category: Brd2]]
		+	[[Category: Bromodomain]]
		+	[[Category: Bromodomain containing protein 2]]
		+	[[Category: Epigenetic reader]]
		+	[[Category: Histone]]
		+	[[Category: Inhibitor]]
		+	[[Category: Transcription]]

OCA at 11:12, 29 July 2020

2020-07-29T11:12:15Z

←Older revision		Revision as of 11:12, 29 July 2020
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-	'''Unreleased structure'''

-	~~The entry 6z7f is ON HOLD until Paper Publication~~	+	==C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-acetamido-3-(benzyloxy)benzamide==
-		+	<StructureSection load='6z7f' size='340' side='right'caption='[[6z7f]]' scene=''>
-	~~Authors: Chung, C.~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6Z7F OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6Z7F FirstGlance]. <br>
-	~~Description:~~ C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-acetamido-3-(benzyloxy)benzamide	+	</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=6z7f FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6z7f OCA], [http://pdbe.org/6z7f PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6z7f RCSB], [http://www.ebi.ac.uk/pdbsum/6z7f PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6z7f ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	</table>
-	[[Category: Chung, C]]	+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Chung C]]

OCA: Protected "6z7f" [edit=sysop:move=sysop]

2020-06-10T05:07:51Z

Protected "6z7f" [edit=sysop:move=sysop]

←Older revision

Revision as of 05:07, 10 June 2020

OCA: New page: '''Unreleased structure''' The entry 6z7f is ON HOLD until Paper Publication Authors: Chung, C. Description: C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-a...

2020-06-10T05:07:49Z

New page: '''Unreleased structure''' The entry 6z7f is ON HOLD until Paper Publication Authors: Chung, C. Description: C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-a...

New page

'''Unreleased structure'''

The entry 6z7f is ON HOLD until Paper Publication

Authors: Chung, C.

Description: C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-acetamido-3-(benzyloxy)benzamide
[[Category: Unreleased Structures]]
[[Category: Chung, C]]

6z7f - Revision history

OCA at 07:12, 2 September 2020

OCA at 11:12, 29 July 2020

OCA: Protected "6z7f" [edit=sysop:move=sysop]

OCA: New page: '''Unreleased structure''' The entry 6z7f is ON HOLD until Paper Publication Authors: Chung, C. Description: C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-a...