6g0p - Revision history

OCA at 08:41, 26 December 2018

OCA — Wed, 26 Dec 2018 08:41:10 GMT

←Older revision		Revision as of 08:41, 26 December 2018
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	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity). [[http://www.uniprot.org/uniprot/E2F1_HUMAN E2F1_HUMAN]] Transcription activator that binds DNA cooperatively with DP proteins through the E2 recognition site, 5'-TTTC[CG]CGC-3' found in the promoter region of a number of genes whose products are involved in cell cycle regulation or in DNA replication. The DRTF1/E2F complex functions in the control of cell-cycle progression from G1 to S phase. E2F1 binds preferentially RB1 in a cell-cycle dependent manner. It can mediate both cell proliferation and TP53/p53-dependent apoptosis.<ref>PMID:8170954</ref> <ref>PMID:10675335</ref> <ref>PMID:12717439</ref> <ref>PMID:17704056</ref>		[[http://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity). [[http://www.uniprot.org/uniprot/E2F1_HUMAN E2F1_HUMAN]] Transcription activator that binds DNA cooperatively with DP proteins through the E2 recognition site, 5'-TTTC[CG]CGC-3' found in the promoter region of a number of genes whose products are involved in cell cycle regulation or in DNA replication. The DRTF1/E2F complex functions in the control of cell-cycle progression from G1 to S phase. E2F1 binds preferentially RB1 in a cell-cycle dependent manner. It can mediate both cell proliferation and TP53/p53-dependent apoptosis.<ref>PMID:8170954</ref> <ref>PMID:10675335</ref> <ref>PMID:12717439</ref> <ref>PMID:17704056</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Targeting bromodomains (BRDs) of the bromo-and-extra-terminal (BET) family offers opportunities for therapeutic intervention in cancer and other diseases. Here, we profile the interactomes of BRD2, BRD3, BRD4, and BRDT following treatment with the pan-BET BRD inhibitor JQ1, revealing broad rewiring of the interaction landscape, with three distinct classes of behavior for the 603 unique interactors identified. A group of proteins associate in a JQ1-sensitive manner with BET BRDs through canonical and new binding modes, while two classes of extra-terminal (ET)-domain binding motifs mediate acetylation-independent interactions. Last, we identify an unexpected increase in several interactions following JQ1 treatment that define negative functions for BRD3 in the regulation of rRNA synthesis and potentially RNAPII-dependent gene expression that result in decreased cell proliferation. Together, our data highlight the contributions of BET protein modules to their interactomes allowing for a better understanding of pharmacological rewiring in response to JQ1.
		+
		+	Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains.,Lambert JP, Picaud S, Fujisawa T, Hou H, Savitsky P, Uuskula-Reimand L, Gupta GD, Abdouni H, Lin ZY, Tucholska M, Knight JDR, Gonzalez-Badillo B, St-Denis N, Newman JA, Stucki M, Pelletier L, Bandeira N, Wilson MD, Filippakopoulos P, Gingras AC Mol Cell. 2018 Dec 13. pii: S1097-2765(18)30948-1. doi:, 10.1016/j.molcel.2018.11.006. PMID:30554943<ref>PMID:30554943</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 6g0p" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 20:30, 2 December 2018

OCA — Sun, 02 Dec 2018 20:30:44 GMT

←Older revision		Revision as of 20:30, 2 December 2018
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-	'''Unreleased structure'''

-	~~The entry~~ 6g0p ~~is ON HOLD~~	+	==Crystal Structure of the first bromodomain of human BRD4 in complex with an acetylated E2F1 peptide (K117ac/K120ac)==
-		+	<StructureSection load='6g0p' size='340' side='right' caption='[[6g0p]], [[Resolution\|resolution]] 1.30Å' scene=''>
-	~~Authors~~: ~~Filippakopoulos, P~~.~~, Picaud, S~~.~~, Krojer, T~~., ~~Sorrell~~, F., ~~Pike, A~~.C.W., ~~von Delft~~, F., ~~Arrowsmith, C~~.H., ~~Edwards, A~~.M., ~~Bountra~~, C.	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[6g0p]] is a 2 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=6G0P OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6G0P FirstGlance]. <br>
-	~~Description~~: ~~Crystal Structure of~~ the ~~first bromodomain~~ of ~~human BRD4~~ in complex ~~with an acetylated~~ E2F1 ~~peptide (K117ac~~/~~K120ac)~~	+	</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></td></tr>
-	[[Category: ~~Unreleased Structures~~]]	+	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=ALY:N(6)-ACETYLLYSINE'>ALY</scene></td></tr>
-	[[Category: ~~Pike~~, A.C.W]]	+	<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>
-	[[Category: ~~Arrowsmith~~, C.H]]	+	<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=6g0p FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6g0p OCA], [http://pdbe.org/6g0p PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6g0p RCSB], [http://www.ebi.ac.uk/pdbsum/6g0p PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6g0p ProSAT]</span></td></tr>
-	[[Category: ~~Von~~ Delft, F]]	+	</table>
-	[[Category: ~~Picaud~~, S]]	+	== 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). [[http://www.uniprot.org/uniprot/E2F1_HUMAN E2F1_HUMAN]] Transcription activator that binds DNA cooperatively with DP proteins through the E2 recognition site, 5'-TTTC[CG]CGC-3' found in the promoter region of a number of genes whose products are involved in cell cycle regulation or in DNA replication. The DRTF1/E2F complex functions in the control of cell-cycle progression from G1 to S phase. E2F1 binds preferentially RB1 in a cell-cycle dependent manner. It can mediate both cell proliferation and TP53/p53-dependent apoptosis.<ref>PMID:8170954</ref> <ref>PMID:10675335</ref> <ref>PMID:12717439</ref> <ref>PMID:17704056</ref>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Human]]
		+	[[Category: Arrowsmith, C H]]
		+	[[Category: Bountra, C]]
		+	[[Category: Delft, F von]]
		+	[[Category: Edwards, A M]]
	[[Category: Filippakopoulos, P]]		[[Category: Filippakopoulos, P]]
-	[[Category: Edwards, A.M]]
	[[Category: Krojer, T]]		[[Category: Krojer, T]]
-	[[Category: ~~Bountra~~, C]]	+	[[Category: Picaud, S]]
		+	[[Category: Pike, A C.W]]
	[[Category: Sorrell, F]]		[[Category: Sorrell, F]]
		+	[[Category: Bromodomain]]
		+	[[Category: Complex]]
		+	[[Category: Transcription]]

OCA: Protected "6g0p" [edit=sysop:move=sysop]

OCA — Wed, 28 Mar 2018 05:27:39 GMT

Protected "6g0p" [edit=sysop:move=sysop]

←Older revision

Revision as of 05:27, 28 March 2018

OCA: New page: '''Unreleased structure''' The entry 6g0p is ON HOLD Authors: Filippakopoulos, P., Picaud, S., Krojer, T., Sorrell, F., Pike, A.C.W., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bou...

OCA — Wed, 28 Mar 2018 05:27:38 GMT

New page: '''Unreleased structure''' The entry 6g0p is ON HOLD Authors: Filippakopoulos, P., Picaud, S., Krojer, T., Sorrell, F., Pike, A.C.W., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bou...

New page

'''Unreleased structure'''

The entry 6g0p is ON HOLD

Authors: Filippakopoulos, P., Picaud, S., Krojer, T., Sorrell, F., Pike, A.C.W., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bountra, C.

Description: Crystal Structure of the first bromodomain of human BRD4 in complex with an acetylated E2F1 peptide (K117ac/K120ac)
[[Category: Unreleased Structures]]
[[Category: Pike, A.C.W]]
[[Category: Arrowsmith, C.H]]
[[Category: Von Delft, F]]
[[Category: Picaud, S]]
[[Category: Filippakopoulos, P]]
[[Category: Edwards, A.M]]
[[Category: Krojer, T]]
[[Category: Bountra, C]]
[[Category: Sorrell, F]]