5igl - Revision history

OCA at 13:51, 30 August 2023

OCA — Wed, 30 Aug 2023 13:51:47 GMT

←Older revision		Revision as of 13:51, 30 August 2023
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	<StructureSection load='5igl' size='340' side='right'caption='[[5igl]], [[Resolution\|resolution]] 2.10Å' scene=''>		<StructureSection load='5igl' size='340' side='right'caption='[[5igl]], [[Resolution\|resolution]] 2.10Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5igl]] 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=5IGL OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=5IGL FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5igl]] is a 1 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=5IGL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5IGL FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat" id="~~ligandDat~~">~~<scene name='pdbligand=BMF:BROMOSPORINE'>BMF</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]] 2.1Å</td></tr>
-	<tr id='~~gene~~'><td class="sblockLbl"><b>[[~~Gene~~\|~~Gene~~:]]</b></td><td class="sblockDat">~~TAF1L ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode~~=~~Info&srchmode~~=~~5&id=9606 HUMAN])~~</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BMF:BROMOSPORINE'>BMF</scene></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=5igl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5igl OCA], [~~http~~://pdbe.org/5igl PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5igl RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5igl PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5igl 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=5igl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5igl OCA], [https://pdbe.org/5igl PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5igl RCSB], [https://www.ebi.ac.uk/pdbsum/5igl PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5igl ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/TAF1L_HUMAN TAF1L_HUMAN]] May act as a functional substitute for TAF1/TAFII250 during male meiosis, when sex chromosomes are transcriptionally silenced.<ref>PMID:12217962</ref>	+	[https://www.uniprot.org/uniprot/TAF1L_HUMAN TAF1L_HUMAN] May act as a functional substitute for TAF1/TAFII250 during male meiosis, when sex chromosomes are transcriptionally silenced.<ref>PMID:12217962</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 23:		Line 23:
	__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: Delft, F von~~]]	+	[[Category: Edwards AM]]
-	[[Category: Edwards~~, A M~~]]	+	[[Category: Felletar I]]
-	[[Category: Felletar, I]]	+	[[Category: Filippakopoulos P]]
-	[[Category: Filippakopoulos, P]]	+	[[Category: Knapp S]]
-	[[Category: Knapp, S]]	+	[[Category: Krojer T]]
-	[[Category: Krojer, T]]	+	[[Category: Picaud S]]
-	[[Category: Picaud, S]]	+	[[Category: Tallant C]]
-	~~[[Category: Structural genomic~~]]	+	[[Category: Von Delft F]]
-	[[Category: Tallant, C]]	+
-	[[Category: ~~Sgc]]~~	+
-	~~[[Category: Taf1/tafii250]]~~	+
-	~~[[Category: Transcription~~]]	+

OCA at 07:17, 3 June 2020

OCA — Wed, 03 Jun 2020 07:17:55 GMT

←Older revision		Revision as of 07:17, 3 June 2020
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	==Crystal structure of the second bromodomain of human TAF1L in complex with bromosporine (BSP)==		==Crystal structure of the second bromodomain of human TAF1L in complex with bromosporine (BSP)==
-	<StructureSection load='5igl' size='340' side='right' caption='[[5igl]], [[Resolution\|resolution]] 2.10Å' scene=''>	+	<StructureSection load='5igl' size='340' side='right'caption='[[5igl]], [[Resolution\|resolution]] 2.10Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5igl]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5IGL OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5IGL FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5igl]] 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=5IGL OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5IGL FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=BMF:BROMOSPORINE'>BMF</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BMF:BROMOSPORINE'>BMF</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=5igl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5igl OCA], [http://pdbe.org/5igl PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5igl RCSB], [http://www.ebi.ac.uk/pdbsum/5igl PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5igl ProSAT]</span></td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">TAF1L ([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=5igl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5igl OCA], [http://pdbe.org/5igl PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5igl RCSB], [http://www.ebi.ac.uk/pdbsum/5igl PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5igl ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 22:		Line 23:
	__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 10:58, 2 November 2016

OCA — Wed, 02 Nov 2016 10:58:28 GMT

←Older revision		Revision as of 10:58, 2 November 2016
Line 9:		Line 9:
	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/TAF1L_HUMAN TAF1L_HUMAN]] May act as a functional substitute for TAF1/TAFII250 during male meiosis, when sex chromosomes are transcriptionally silenced.<ref>PMID:12217962</ref>		[[http://www.uniprot.org/uniprot/TAF1L_HUMAN TAF1L_HUMAN]] May act as a functional substitute for TAF1/TAFII250 during male meiosis, when sex chromosomes are transcriptionally silenced.<ref>PMID:12217962</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Bromodomains (BRDs) have emerged as compelling targets for cancer therapy. The development of selective and potent BET (bromo and extra-terminal) inhibitors and their significant activity in diverse tumor models have rapidly translated into clinical studies and have motivated drug development efforts targeting non-BET BRDs. However, the complex multidomain/subunit architecture of BRD protein complexes complicates predictions of the consequences of their pharmacological targeting. To address this issue, we developed a promiscuous BRD inhibitor [bromosporine (BSP)] that broadly targets BRDs (including BETs) with nanomolar affinity, creating a tool for the identification of cellular processes and diseases where BRDs have a regulatory function. As a proof of principle, we studied the effects of BSP on leukemic cell lines known to be sensitive to BET inhibition and found, as expected, strong antiproliferative activity. Comparison of the modulation of transcriptional profiles by BSP after a short exposure to the inhibitor resulted in a BET inhibitor signature but no significant additional changes in transcription that could account for inhibition of other BRDs. Thus, nonselective targeting of BRDs identified BETs, but not other BRDs, as master regulators of context-dependent primary transcription response.
		+
		+	Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.,Picaud S, Leonards K, Lambert JP, Dovey O, Wells C, Fedorov O, Monteiro O, Fujisawa T, Wang CY, Lingard H, Tallant C, Nikbin N, Guetzoyan L, Ingham R, Ley SV, Brennan P, Muller S, Samsonova A, Gingras AC, Schwaller J, Vassiliou G, Knapp S, Filippakopoulos P Sci Adv. 2016 Oct 12;2(10):e1600760. eCollection 2016 Oct. PMID:27757418<ref>PMID:27757418</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 5igl" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 00:58, 20 October 2016

OCA — Thu, 20 Oct 2016 00:58:48 GMT

←Older revision		Revision as of 00:58, 20 October 2016
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry 5igl is ON HOLD until Paper Publication~~	+	==Crystal structure of the second bromodomain of human TAF1L in complex with bromosporine (BSP)==
-		+	<StructureSection load='5igl' size='340' side='right' caption='[[5igl]], [[Resolution\|resolution]] 2.10Å' scene=''>
-	~~Authors: Filippakopoulos, P., Picaud, S., Felletar, I., Krojer, T., Tallant, C., von Delft, F., Edwards, A.M., Arrowsmith, C.H., Bountra, C., Knapp, S., Structural Genomics Consortium (SGC)~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[5igl]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5IGL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5IGL FirstGlance]. <br>
-	~~Description:~~ Crystal structure of the second bromodomain of human TAF1L in complex with bromosporine (BSP)	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=BMF:BROMOSPORINE'>BMF</scene></td></tr>
-	[[~~Category~~: ~~Unreleased Structures~~]]	+	<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=5igl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5igl OCA], [http://pdbe.org/5igl PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5igl RCSB], [http://www.ebi.ac.uk/pdbsum/5igl PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5igl ProSAT]</span></td></tr>
-	[[~~Category~~: ~~Picaud, S~~]]	+	</table>
-	[[~~Category~~: ~~Knapp~~, S]]	+	== Function ==
-	[[Category: ~~Krojer~~, T]]	+	[[http://www.uniprot.org/uniprot/TAF1L_HUMAN TAF1L_HUMAN]] May act as a functional substitute for TAF1/TAFII250 during male meiosis, when sex chromosomes are transcriptionally silenced.<ref>PMID:12217962</ref>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Arrowsmith, C H]]
	[[Category: Bountra, C]]		[[Category: Bountra, C]]
		+	[[Category: Delft, F von]]
		+	[[Category: Edwards, A M]]
	[[Category: Felletar, I]]		[[Category: Felletar, I]]
-	[[Category: Arrowsmith, C.H]]
-	[[Category: Von Delft, F]]
	[[Category: Filippakopoulos, P]]		[[Category: Filippakopoulos, P]]
-	[[Category: ~~Edwards~~, ~~A.M~~]]	+	[[Category: Knapp, S]]
-	[[Category: Structural ~~Genomics Consortium (Sgc)~~]]	+	[[Category: Krojer, T]]
		+	[[Category: Picaud, S]]
		+	[[Category: Structural genomic]]
	[[Category: Tallant, C]]		[[Category: Tallant, C]]
		+	[[Category: Sgc]]
		+	[[Category: Taf1/tafii250]]
		+	[[Category: Transcription]]

OCA: Protected "5igl" [edit=sysop:move=sysop]

OCA — Thu, 10 Mar 2016 02:17:00 GMT

Protected "5igl" [edit=sysop:move=sysop]

←Older revision

Revision as of 02:17, 10 March 2016

OCA: New page: '''Unreleased structure''' The entry 5igl is ON HOLD until Paper Publication Authors: Filippakopoulos, P., Picaud, S., Felletar, I., Krojer, T., Tallant, C., von Delft, F., Edwards, A.M...

OCA — Thu, 10 Mar 2016 02:16:59 GMT

New page: '''Unreleased structure''' The entry 5igl is ON HOLD until Paper Publication Authors: Filippakopoulos, P., Picaud, S., Felletar, I., Krojer, T., Tallant, C., von Delft, F., Edwards, A.M...

New page

'''Unreleased structure'''

The entry 5igl is ON HOLD until Paper Publication

Authors: Filippakopoulos, P., Picaud, S., Felletar, I., Krojer, T., Tallant, C., von Delft, F., Edwards, A.M., Arrowsmith, C.H., Bountra, C., Knapp, S., Structural Genomics Consortium (SGC)

Description: Crystal structure of the second bromodomain of human TAF1L in complex with bromosporine (BSP)
[[Category: Unreleased Structures]]
[[Category: Picaud, S]]
[[Category: Knapp, S]]
[[Category: Krojer, T]]
[[Category: Bountra, C]]
[[Category: Felletar, I]]
[[Category: Arrowsmith, C.H]]
[[Category: Von Delft, F]]
[[Category: Filippakopoulos, P]]
[[Category: Edwards, A.M]]
[[Category: Structural Genomics Consortium (Sgc)]]
[[Category: Tallant, C]]