5hcl: Difference between revisions
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New page: '''Unreleased structure''' The entry 5hcl is ON HOLD until Jan 04 2018 Authors: Dong, J., Weber, F.E., Caflisch, A. Description: Crystal Structure of the first bromodomain of BRD4 in c... |
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==Crystal Structure of the first bromodomain of BRD4 in complex with DMA== | |||
<StructureSection load='5hcl' size='340' side='right'caption='[[5hcl]], [[Resolution|resolution]] 1.50Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[5hcl]] 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=5HCL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5HCL FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.5Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=5Y9:~{N},~{N}-DIMETHYLETHANAMIDE'>5Y9</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</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=5hcl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5hcl OCA], [https://pdbe.org/5hcl PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5hcl RCSB], [https://www.ebi.ac.uk/pdbsum/5hcl PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5hcl ProSAT]</span></td></tr> | |||
</table> | |||
== Disease == | |||
[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> | |||
== Function == | |||
[https://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity). | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
N,N-Dimethylacetamide (DMA) is a water-miscible solvent, FDA approved as excipient and therefore widely used as drug-delivery vehicle. As such, DMA should be devoid of any bioactivity. Here we report that DMA is epigenetically active since it binds bromodomains and inhibits osteoclastogenesis and inflammation. Moreover, DMA enhances bone regeneration in vivo. Therefore, our in vivo and in vitro data reveal DMA's potential as an anti-osteoporotic agent via the inhibition of osteoclast mediated bone resorption and enhanced bone regeneration. Our results highlight the potential therapeutic benefits of DMA and the need for reconsideration of previous reports where DMA was used as an 'inactive' drug-delivery vehicle. | |||
N,N Dimethylacetamide a drug excipient that acts as bromodomain ligand for osteoporosis treatment.,Ghayor C, Gjoksi B, Dong J, Siegenthaler B, Caflisch A, Weber FE Sci Rep. 2017 Feb 8;7:42108. doi: 10.1038/srep42108. PMID:28176838<ref>PMID:28176838</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
[[Category: | <div class="pdbe-citations 5hcl" style="background-color:#fffaf0;"></div> | ||
[[Category: Caflisch | |||
[[Category: Weber | ==See Also== | ||
*[[Bromodomain-containing protein 3D structures|Bromodomain-containing protein 3D structures]] | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Homo sapiens]] | |||
[[Category: Large Structures]] | |||
[[Category: Caflisch A]] | |||
[[Category: Dong J]] | |||
[[Category: Weber FE]] | |||
Latest revision as of 10:31, 9 August 2023
Crystal Structure of the first bromodomain of BRD4 in complex with DMACrystal Structure of the first bromodomain of BRD4 in complex with DMA
Structural highlights
DiseaseBRD4_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.[1] [2] FunctionBRD4_HUMAN Plays a role in a process governing chromosomal dynamics during mitosis (By similarity). Publication Abstract from PubMedN,N-Dimethylacetamide (DMA) is a water-miscible solvent, FDA approved as excipient and therefore widely used as drug-delivery vehicle. As such, DMA should be devoid of any bioactivity. Here we report that DMA is epigenetically active since it binds bromodomains and inhibits osteoclastogenesis and inflammation. Moreover, DMA enhances bone regeneration in vivo. Therefore, our in vivo and in vitro data reveal DMA's potential as an anti-osteoporotic agent via the inhibition of osteoclast mediated bone resorption and enhanced bone regeneration. Our results highlight the potential therapeutic benefits of DMA and the need for reconsideration of previous reports where DMA was used as an 'inactive' drug-delivery vehicle. N,N Dimethylacetamide a drug excipient that acts as bromodomain ligand for osteoporosis treatment.,Ghayor C, Gjoksi B, Dong J, Siegenthaler B, Caflisch A, Weber FE Sci Rep. 2017 Feb 8;7:42108. doi: 10.1038/srep42108. PMID:28176838[3] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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