OCA at 13:36, 1 February 2024

OCA — Thu, 01 Feb 2024 13:36:46 GMT

←Older revision		Revision as of 13:36, 1 February 2024
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	==Crystal structure of BRD9 bromodomain in complex with compound EA-89==		==Crystal structure of BRD9 bromodomain in complex with compound EA-89==
-	<StructureSection load='8a7i' size='340' side='right'caption='[[8a7i]]' scene=''>	+	<StructureSection load='8a7i' size='340' side='right'caption='[[8a7i]], [[Resolution\|resolution]] 1.76Å' 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=8A7I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8A7I FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[8a7i]] is a 2 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=8A7I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8A7I 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=8a7i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8a7i OCA], [https://pdbe.org/8a7i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8a7i RCSB], [https://www.ebi.ac.uk/pdbsum/8a7i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8a7i 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]] 1.76Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=L8L:~{N}-[1,1-bis(oxidanylidene)thian-4-yl]-7-[3-methyl-1-(piperidin-4-ylmethyl)indol-5-yl]-4-oxidanylidene-5-propyl-thieno[3,2-c]pyridine-2-carboxamide'>L8L</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=8a7i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8a7i OCA], [https://pdbe.org/8a7i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8a7i RCSB], [https://www.ebi.ac.uk/pdbsum/8a7i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8a7i ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[https://www.uniprot.org/uniprot/BRD9_HUMAN BRD9_HUMAN] May play a role in chromatin remodeling and regulation of transcription.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Bromodomain-containing protein 9 (BRD9), an essential component of the SWI/SNF chromatin remodeling complex termed ncBAF, has been established as a therapeutic target in a subset of sarcomas and leukemias. Here, we used novel small molecule inhibitors and degraders along with RNA interference to assess the dependency on BRD9 in the context of diverse hematological malignancies, including acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL), and multiple myeloma (MM) model systems. Following depletion of BRD9 protein, AML cells undergo terminal differentiation, whereas apoptosis was more prominent in ALL and MM. RNA-seq analysis of acute leukemia and MM cells revealed both unique and common signaling pathways affected by BRD9 degradation, with common pathways including those associated with regulation of inflammation, cell adhesion, DNA repair and cell cycle progression. Degradation of BRD9 potentiated the effects of several chemotherapeutic agents and targeted therapies against AML, ALL, and MM. Our findings support further development of therapeutic targeting of BRD9, alone or combined with other agents, as a novel strategy for acute leukemias and MM.
		+
		+	BRD9 degraders as chemosensitizers in acute leukemia and multiple myeloma.,Weisberg E, Chowdhury B, Meng C, Case AE, Ni W, Garg S, Sattler M, Azab AK, Sun J, Muz B, Sanchez D, Toure A, Stone RM, Galinsky I, Winer E, Gleim S, Gkountela S, Kedves A, Harrington E, Abrams T, Zoller T, Vaupel A, Manley P, Faller M, Chung B, Chen X, Busenhart P, Stephan C, Calkins K, Bonenfant D, Thoma CR, Forrester W, Griffin JD Blood Cancer J. 2022 Jul 19;12(7):110. doi: 10.1038/s41408-022-00704-7. PMID:35853853<ref>PMID:35853853</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 8a7i" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Faller M]]		[[Category: Faller M]]
	[[Category: Zink F]]		[[Category: Zink F]]

OCA at 05:03, 10 August 2022

OCA — Wed, 10 Aug 2022 05:03:48 GMT

←Older revision		Revision as of 05:03, 10 August 2022
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 8a7i ~~is ON HOLD until Paper Publication~~	+	==Crystal structure of BRD9 bromodomain in complex with compound EA-89==
-		+	<StructureSection load='8a7i' size='340' side='right'caption='[[8a7i]]' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8A7I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8A7I 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=8a7i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8a7i OCA], [https://pdbe.org/8a7i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8a7i RCSB], [https://www.ebi.ac.uk/pdbsum/8a7i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8a7i ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	</table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Faller M]]
		+	[[Category: Zink F]]

OCA: Protected "8a7i" [edit=sysop:move=sysop]

OCA — Wed, 29 Jun 2022 06:22:13 GMT

Protected "8a7i" [edit=sysop:move=sysop]

←Older revision

Revision as of 06:22, 29 June 2022

OCA: New page: '''Unreleased structure''' The entry 8a7i is ON HOLD until Paper Publication Authors: Description: Category: Unreleased Structures

OCA — Wed, 29 Jun 2022 06:22:12 GMT

New page: '''Unreleased structure''' The entry 8a7i is ON HOLD until Paper Publication Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 8a7i is ON HOLD until Paper Publication

Authors:

Description:
[[Category: Unreleased Structures]]

8a7i - Revision history

OCA at 13:36, 1 February 2024

OCA at 05:03, 10 August 2022

OCA: Protected "8a7i" [edit=sysop:move=sysop]

OCA: New page: '''Unreleased structure''' The entry 8a7i is ON HOLD until Paper Publication Authors: Description: Category: Unreleased Structures