4tyl: Difference between revisions
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==Fragment-Based Screening of the Bromodomain of ATAD2== | ==Fragment-Based Screening of the Bromodomain of ATAD2== | ||
<StructureSection load='4tyl' size='340' side='right' caption='[[4tyl]], [[Resolution|resolution]] 1.85Å' scene=''> | <StructureSection load='4tyl' size='340' side='right'caption='[[4tyl]], [[Resolution|resolution]] 1.85Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4tyl]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4TYL OCA]. For a <b>guided tour on the structure components</b> use [ | <table><tr><td colspan='2'>[[4tyl]] 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=4TYL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4TYL FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=39O:5-AMINO-1,3,6-TRIMETHYL-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE'>39O</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.85Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=39O:5-AMINO-1,3,6-TRIMETHYL-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE'>39O</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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=4tyl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4tyl OCA], [https://pdbe.org/4tyl PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4tyl RCSB], [https://www.ebi.ac.uk/pdbsum/4tyl PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4tyl ProSAT]</span></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | |||
</table> | </table> | ||
== Function == | == Function == | ||
[ | [https://www.uniprot.org/uniprot/ATAD2_HUMAN ATAD2_HUMAN] May be a transcriptional coactivator of the nuclear receptor ESR1 required to induce the expression of a subset of estradiol target genes, such as CCND1, MYC and E2F1. May play a role in the recruitment or occupancy of CREBBP at some ESR1 target gene promoters. May be required for histone hyperacetylation. Involved in the estrogen-induced cell proliferation and cell cycle progression of breast cancer cells.<ref>PMID:17998543</ref> | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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</div> | </div> | ||
<div class="pdbe-citations 4tyl" style="background-color:#fffaf0;"></div> | <div class="pdbe-citations 4tyl" style="background-color:#fffaf0;"></div> | ||
==See Also== | |||
*[[ATPase family AAA domain-containing protein|ATPase family AAA domain-containing protein]] | |||
*[[ATPase family AAA domain-containing protein 2|ATPase family AAA domain-containing protein 2]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Homo sapiens]] | ||
[[Category: | [[Category: Large Structures]] | ||
[[Category: | [[Category: Chauder BA]] | ||
[[Category: | [[Category: Fesik SW]] | ||
[[Category: | [[Category: Harner MJ]] | ||
[[Category: | [[Category: Phan J]] | ||
Latest revision as of 03:48, 28 December 2023
Fragment-Based Screening of the Bromodomain of ATAD2Fragment-Based Screening of the Bromodomain of ATAD2
Structural highlights
FunctionATAD2_HUMAN May be a transcriptional coactivator of the nuclear receptor ESR1 required to induce the expression of a subset of estradiol target genes, such as CCND1, MYC and E2F1. May play a role in the recruitment or occupancy of CREBBP at some ESR1 target gene promoters. May be required for histone hyperacetylation. Involved in the estrogen-induced cell proliferation and cell cycle progression of breast cancer cells.[1] Publication Abstract from PubMedCellular and genetic evidence suggest that inhibition of ATAD2 could be a useful strategy to treat several types of cancer. To discover small molecule inhibitors of the bromodomain of ATAD2, we used a fragment-based approach. Fragment hits were identified using NMR spectroscopy, and ATAD2 was crystallized with three of the hits identified in the fragment screen. Fragment-based screening of the bromodomain of ATAD2.,Harner MJ, Chauder BA, Phan J, Fesik SW J Med Chem. 2014 Oct 14. PMID:25314628[2] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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