OCA at 15:10, 18 October 2023

2023-10-18T15:10:56Z

←Older revision		Revision as of 15:10, 18 October 2023
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	==Crystal Structure of BPTF bromodomain labelled with 5-fluoro-tryptophan==		==Crystal Structure of BPTF bromodomain labelled with 5-fluoro-tryptophan==
-	<StructureSection load='7jt4' size='340' side='right'caption='[[7jt4]]' scene=''>	+	<StructureSection load='7jt4' size='340' side='right'caption='[[7jt4]], [[Resolution\|resolution]] 2.06Å' 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=7JT4 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7JT4 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[7jt4]] 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=7JT4 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7JT4 FirstGlance]. <br>
-	</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=7jt4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7jt4 OCA], [https://pdbe.org/7jt4 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7jt4 RCSB], [https://www.ebi.ac.uk/pdbsum/7jt4 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7jt4 ProSAT]</span></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]] 2.06Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=FTR:FLUOROTRYPTOPHANE'>FTR</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=7jt4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7jt4 OCA], [https://pdbe.org/7jt4 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7jt4 RCSB], [https://www.ebi.ac.uk/pdbsum/7jt4 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7jt4 ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[https://www.uniprot.org/uniprot/BPTF_HUMAN BPTF_HUMAN] Histone-binding component of NURF (nucleosome-remodeling factor), a complex which catalyzes ATP-dependent nucleosome sliding and facilitates transcription of chromatin. Specifically recognizes H3 tails trimethylated on 'Lys-4' (H3K4me3), which mark transcription start sites of virtually all active genes. May also regulate transcription through direct binding to DNA or transcription factors.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Bromodomain and PHD finger containing protein transcription factor (BPTF) is an epigenetic protein involved in chromatin remodelling and is a potential anticancer target. The BPTF bromodomain has one reported small molecule inhibitor (AU1, rac-1). Here, advances made on the structure-activity relationship of a BPTF bromodomain ligand are reported using a combination of experimental and molecular dynamics simulations leading to the active enatiomer (S)-1. Additionally, a ligand deconstruction analysis was conducted to characterize important pharmacophores for engaging the BPTF bromodomain. These studies have been enabled by a protein-based fluorine NMR approach, highlighting the versatility of the method for selectivity, ligand deconstruction, and ligand binding. To enable future analysis of biological activity, cell growth analyses in a panel of cancer cell lines were carried out using CRISPR-Cas9 and (S)-1 to identify cell-based model systems that are sensitive to BPTF inhibition.
		+
		+	Selectivity, ligand deconstruction, and cellular activity analysis of a BPTF bromodomain inhibitor.,Kirberger SE, Ycas PD, Johnson JA, Chen C, Ciccone MF, Woo RWL, Urick AK, Zahid H, Shi K, Aihara H, McAllister SD, Kashani-Sabet M, Shi J, Dickson A, Dos Santos CO, Pomerantz WCK Org Biomol Chem. 2019 Feb 13;17(7):2020-2027. doi: 10.1039/c8ob02599a. PMID:30706071<ref>PMID:30706071</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 7jt4" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Aihara H]]		[[Category: Aihara H]]

OCA at 10:33, 28 July 2021

2021-07-28T10:33:22Z

←Older revision		Revision as of 10:33, 28 July 2021
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-	'''Unreleased structure'''

-	~~The entry~~ 7jt4 is ~~ON HOLD~~	+	==Crystal Structure of BPTF bromodomain labelled with 5-fluoro-tryptophan==
-		+	<StructureSection load='7jt4' size='340' side='right'caption='[[7jt4]]' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7JT4 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7JT4 FirstGlance]. <br>
-	~~Description~~:	+	</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=7jt4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7jt4 OCA], [https://pdbe.org/7jt4 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7jt4 RCSB], [https://www.ebi.ac.uk/pdbsum/7jt4 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7jt4 ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased Structures~~]]	+	</table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Aihara H]]
		+	[[Category: Johnson JA]]
		+	[[Category: Pomerantz WCK]]
		+	[[Category: Shi K]]

OCA: Protected "7jt4" [edit=sysop:move=sysop]

2020-08-26T09:37:37Z

Protected "7jt4" [edit=sysop:move=sysop]

←Older revision

Revision as of 09:37, 26 August 2020

OCA: New page: '''Unreleased structure''' The entry 7jt4 is ON HOLD Authors: Description: Category: Unreleased Structures

2020-08-26T09:37:35Z

New page: '''Unreleased structure''' The entry 7jt4 is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 7jt4 is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]

7jt4 - Revision history

OCA at 15:10, 18 October 2023

OCA at 10:33, 28 July 2021

OCA: Protected "7jt4" [edit=sysop:move=sysop]

OCA: New page: '''Unreleased structure''' The entry 7jt4 is ON HOLD Authors: Description: Category: Unreleased Structures