7p6y

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==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH compound 5ef==
==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH compound 5ef==
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<StructureSection load='7p6y' size='340' side='right'caption='[[7p6y]]' scene=''>
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<StructureSection load='7p6y' size='340' side='right'caption='[[7p6y]], [[Resolution|resolution]] 1.88&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7P6Y OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7P6Y FirstGlance]. <br>
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<table><tr><td colspan='2'>[[7p6y]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7P6Y OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7P6Y FirstGlance]. <br>
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</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=7p6y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7p6y OCA], [https://pdbe.org/7p6y PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7p6y RCSB], [https://www.ebi.ac.uk/pdbsum/7p6y PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7p6y ProSAT]</span></td></tr>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=5Z1:4-benzoyl-N-(2-(2-(2-((2-(1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)-1-((tetrahydro-2H-pyran-4-yl)methyl)-1H-benzo[d]imidazol-6-yl)(methyl)amino)ethoxy)ethoxy)ethyl)-N-(2-oxo-2-((2-(2-(prop-2-yn-1-yloxy)ethoxy)ethyl)amino)ethyl)benzamide'>5Z1</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[7p6v|7p6v]], [[7p6w|7p6w]]</div></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7p6y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7p6y OCA], [https://pdbe.org/7p6y PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7p6y RCSB], [https://www.ebi.ac.uk/pdbsum/7p6y PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7p6y ProSAT]</span></td></tr>
</table>
</table>
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== Disease ==
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[[https://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>
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== Function ==
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[[https://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity).
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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We present a one-step Ugi reaction protocol for the expedient synthesis of photoaffinity probes for live-cell MS-based proteomics. The reaction couples an amine affinity function with commonly used photoreactive groups, and a variety of handle functionalities. Using this technology, a series of pan-BET (BET: bromodomain and extra-terminal domain) selective bromodomain photoaffinity probes were obtained by parallel synthesis. Studies on the effects of photoreactive group, linker length and irradiation wavelength on photocrosslinking efficiency provide valuable insights into photoaffinity probe design. Optimal probes were progressed to MS-based proteomics to capture the BET family of proteins from live cells and reveal their potential on- and off-target profiles.
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One-Step Synthesis of Photoaffinity Probes for Live-Cell MS-Based Proteomics.,Fallon DJ, Lehmann S, Chung CW, Phillipou A, Eberl C, Fantom KGM, Zappacosta F, Patel VK, Bantscheff M, Schofield CJ, Tomkinson NCO, Bush JT Chemistry. 2021 Jul 30. doi: 10.1002/chem.202102036. PMID:34328642<ref>PMID:34328642</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 7p6y" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Chung C]]
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[[Category: Chung, C]]
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[[Category: Antagonist]]
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[[Category: Brd4]]
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[[Category: Bromodomain]]
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[[Category: Bromodomain containing protein 4]]
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[[Category: Epigenetic reader]]
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[[Category: Histone]]
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[[Category: Inhibitor]]
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[[Category: Transcription]]

Revision as of 14:18, 29 December 2021

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH compound 5ef

PDB ID 7p6y

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