6swp - Revision history

OCA at 06:33, 6 May 2020

2020-05-06T06:33:02Z

←Older revision		Revision as of 06:33, 6 May 2020
Line 3:		Line 3:
	<StructureSection load='6swp' size='340' side='right'caption='[[6swp]], [[Resolution\|resolution]] 1.60Å' scene=''>		<StructureSection load='6swp' size='340' side='right'caption='[[6swp]], [[Resolution\|resolution]] 1.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6swp]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6SWP OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6SWP FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6swp]] 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=6SWP OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6SWP FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=LW5:4-acetamido-3-fluoranyl-~{N}-(4-oxidanylcyclohexyl)-5-[(1~{S})-1-phenylethoxy]benzamide'>LW5</scene></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=LW5:4-acetamido-3-fluoranyl-~{N}-(4-oxidanylcyclohexyl)-5-[(1~{S})-1-phenylethoxy]benzamide'>LW5</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=6swp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6swp OCA], [http://pdbe.org/6swp PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6swp RCSB], [http://www.ebi.ac.uk/pdbsum/6swp PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6swp ProSAT]</span></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=6swp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6swp OCA], [http://pdbe.org/6swp PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6swp RCSB], [http://www.ebi.ac.uk/pdbsum/6swp PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6swp ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 22:		Line 23:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Chung, C]]		[[Category: Chung, C]]

OCA at 09:21, 1 April 2020

2020-04-01T09:21:03Z

←Older revision		Revision as of 09:21, 1 April 2020
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 6swp is ~~ON HOLD~~ ~~until Paper~~ Publication	+	==C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH iBET-BD2 (GSK046)==
		+	<StructureSection load='6swp' size='340' side='right'caption='[[6swp]], [[Resolution\|resolution]] 1.60Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[6swp]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6SWP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6SWP FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=LW5:4-acetamido-3-fluoranyl-~{N}-(4-oxidanylcyclohexyl)-5-[(1~{S})-1-phenylethoxy]benzamide'>LW5</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=6swp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6swp OCA], [http://pdbe.org/6swp PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6swp RCSB], [http://www.ebi.ac.uk/pdbsum/6swp PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6swp ProSAT]</span></td></tr>
		+	</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 ==
		+	The two tandem bromodomains of the BET proteins enable chromatin binding to facilitate transcription. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. To explore the individual functional contributions of the first (BD1) and second (BD2) bromodomains in biology and therapy, we developed selective BD1 and BD2 inhibitors. We found that steady-state gene expression primarily requires BD1 whereas the rapid increase of gene expression induced by inflammatory stimuli requires both BD1 and BD2 of all BET proteins. BD1 inhibitors phenocopied the effects of pan-BET inhibitors in cancer models whereas BD2 inhibitors were predominantly effective in models of inflammatory and autoimmune disease. These insights into the differential requirement of BD1 and BD2 for the maintenance and induction of gene expression may guide future BET targeted therapies.

-	~~Authors:~~ Chung, C.	+	Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation.,Gilan O, Rioja I, Knezevic K, Bell MJ, Yeung MM, Harker NR, Lam EYN, Chung CW, Bamborough P, Petretich M, Urh M, Atkinson SJ, Bassil AK, Roberts EJ, Vassiliadis D, Burr ML, Preston AGS, Wellaway C, Werner T, Gray JR, Michon AM, Gobbetti T, Kumar V, Soden PE, Haynes A, Vappiani J, Tough DF, Taylor S, Dawson SJ, Bantscheff M, Lindon M, Drewes G, Demont EH, Daniels DL, Grandi P, Prinjha RK, Dawson MA Science. 2020 Mar 19. pii: science.aaz8455. doi: 10.1126/science.aaz8455. PMID:32193360<ref>PMID:32193360</ref>

-	~~Description: C~~-~~TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH iBET~~-~~BD2 (GSK046)~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased~~ Structures]]	+	</div>
		+	<div class="pdbe-citations 6swp" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[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 07:14, 25 December 2019

2019-12-25T07:14:39Z

←Older revision		Revision as of 07:14, 25 December 2019
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

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

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

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

2019-10-02T07:56:33Z

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

←Older revision

Revision as of 07:56, 2 October 2019

OCA: New page: '''Unreleased structure''' The entry 6swp is ON HOLD Authors: Chung, C. Description: C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH iBET-BD2 (GSK046) Category: Unreleased Structures [[C...

2019-10-02T07:56:31Z

New page: '''Unreleased structure''' The entry 6swp is ON HOLD Authors: Chung, C. Description: C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH iBET-BD2 (GSK046) Category: Unreleased Structures [[C...

New page

'''Unreleased structure'''

The entry 6swp is ON HOLD

Authors: Chung, C.

Description: C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH iBET-BD2 (GSK046)
[[Category: Unreleased Structures]]
[[Category: Chung, C]]