6z7g - Revision history

OCA at 07:12, 2 September 2020

OCA — Wed, 02 Sep 2020 07:12:56 GMT

←Older revision		Revision as of 07:12, 2 September 2020
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	==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-acetamido-3-(benzyloxy)benzamide==		==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-acetamido-3-(benzyloxy)benzamide==
-	<StructureSection load='6z7g' size='340' side='right'caption='[[6z7g]]' scene=''>	+	<StructureSection load='6z7g' size='340' side='right'caption='[[6z7g]], [[Resolution\|resolution]] 1.59Å' 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=6Z7G OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6Z7G FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6z7g]] 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=6Z7G OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6Z7G 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=6z7g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6z7g OCA], [http://pdbe.org/6z7g PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6z7g RCSB], [http://www.ebi.ac.uk/pdbsum/6z7g PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6z7g 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=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">BRD4, HUNK1 ([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=6z7g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6z7g OCA], [http://pdbe.org/6z7g PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6z7g RCSB], [http://www.ebi.ac.uk/pdbsum/6z7g PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6z7g ProSAT]</span></td></tr>
	</table>		</table>
		+	== Disease ==
		+	[[http://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Note=A chromosomal aberration involving BRD4 is found in a rare, aggressive, and lethal carcinoma arising in midline organs of young people. Translocation t(15;19)(q14;p13) with NUT which produces a BRD4-NUT fusion protein.<ref>PMID:12543779</ref> <ref>PMID:11733348</ref>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity).
		+	<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 6z7g" 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: Brd4]]
		+	[[Category: Bromodomain]]
		+	[[Category: Bromodomain containing protein 4]]
		+	[[Category: Epigenetic reader]]
		+	[[Category: Histone]]
		+	[[Category: Inhibitor]]
		+	[[Category: Transcription]]

OCA at 11:12, 29 July 2020

OCA — Wed, 29 Jul 2020 11:12:14 GMT

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

-	~~The entry 6z7g is ON HOLD until Paper Publication~~	+	==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-acetamido-3-(benzyloxy)benzamide==
-		+	<StructureSection load='6z7g' size='340' side='right'caption='[[6z7g]]' 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=6Z7G OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6Z7G FirstGlance]. <br>
-	~~Description:~~ N-TERMINAL BROMODOMAIN OF HUMAN BRD4 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=6z7g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6z7g OCA], [http://pdbe.org/6z7g PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6z7g RCSB], [http://www.ebi.ac.uk/pdbsum/6z7g PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6z7g ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	</table>
-	[[Category: Chung, C]]	+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Chung C]]

OCA at 11:03, 8 July 2020

OCA — Wed, 08 Jul 2020 11:03:01 GMT

←Older revision		Revision as of 11:03, 8 July 2020
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6z7g is ON HOLD	+	The entry 6z7g is ON HOLD until Paper Publication

	Authors: Chung, C.		Authors: Chung, C.

OCA at 18:35, 24 June 2020

OCA — Wed, 24 Jun 2020 18:35:15 GMT

←Older revision		Revision as of 18:35, 24 June 2020
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6z7g is ON HOLD ~~until Paper Publication~~	+	The entry 6z7g is ON HOLD

	Authors: Chung, C.		Authors: Chung, C.

OCA: Protected "6z7g" [edit=sysop:move=sysop]

OCA — Wed, 10 Jun 2020 05:07:54 GMT

Protected "6z7g" [edit=sysop:move=sysop]

←Older revision

Revision as of 05:07, 10 June 2020

OCA: New page: '''Unreleased structure''' The entry 6z7g is ON HOLD until Paper Publication Authors: Chung, C. Description: N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-a...

OCA — Wed, 10 Jun 2020 05:07:53 GMT

New page: '''Unreleased structure''' The entry 6z7g is ON HOLD until Paper Publication Authors: Chung, C. Description: N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-a...

New page

'''Unreleased structure'''

The entry 6z7g is ON HOLD until Paper Publication

Authors: Chung, C.

Description: N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH N-(2-(1H-imidazol-4-yl)ethyl)-4-acetamido-3-(benzyloxy)benzamide
[[Category: Unreleased Structures]]
[[Category: Chung, C]]