7t3f

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==Development of BRD4 inhibitors as arsenicals antidotes==
==Development of BRD4 inhibitors as arsenicals antidotes==
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<StructureSection load='7t3f' size='340' side='right'caption='[[7t3f]]' scene=''>
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<StructureSection load='7t3f' size='340' side='right'caption='[[7t3f]], [[Resolution|resolution]] 1.28&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=7T3F OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7T3F FirstGlance]. <br>
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<table><tr><td colspan='2'>[[7t3f]] 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=7T3F OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7T3F 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=7t3f FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7t3f OCA], [https://pdbe.org/7t3f PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7t3f RCSB], [https://www.ebi.ac.uk/pdbsum/7t3f PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7t3f ProSAT]</span></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.28&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EM0:4-fluoro-3-methyl-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzene-1-sulfonamide'>EM0</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></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=7t3f FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7t3f OCA], [https://pdbe.org/7t3f PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7t3f RCSB], [https://www.ebi.ac.uk/pdbsum/7t3f PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7t3f 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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Arsenicals belong to the class of chemical warfare agents known as vesicants, which are highly reactive, toxic and cause robust inflammatory response. Cutaneous exposure to arsenicals causes a wide range of systemic organ damage, beginning with cutaneous injuries, and later manifest multi-organ damage and death. Thus, the development of suitable antidotes that can effectively block injury following exposure to these agents is of great importance. Bromodomain 4 (BRD4), a member of the bromodomain and extra terminal domain (BET) family, plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. In this context, the development of potent small molecule inhibitors of BRD4 could serve as potential antidotes for arsenicals. Herein, we describe the synthesis and biological evaluation of a series of compounds.
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Development of BRD4 inhibitors as anti-inflammatory agents and antidotes for arsenicals.,Yatchang MF, Mathew B, Srivastava RK, Khan J, Muzaffar S, Zhang S, Wu M, Zhai L, Ruiz P, Agarwal A, Bostwick JR, Suto MJ, Athar M, Augelli-Szafran CE Bioorg Med Chem Lett. 2022 May 15;64:128696. doi: 10.1016/j.bmcl.2022.128696., Epub 2022 Mar 19. PMID:35318165<ref>PMID:35318165</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 7t3f" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Bromodomain-containing protein 3D structures|Bromodomain-containing protein 3D structures]]
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== References ==
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<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
[[Category: Augelli-Szafran CE]]
[[Category: Augelli-Szafran CE]]

Current revision

Development of BRD4 inhibitors as arsenicals antidotes

PDB ID 7t3f

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