4tz2
From Proteopedia
(Difference between revisions)
(New page: '''Unreleased structure''' The entry 4tz2 is ON HOLD Authors: Harner, M.J., Chauder, B.A., Phan, J., Fesik, S.W. Description:) |
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| - | '''Unreleased structure''' | ||
| - | + | ==Fragment-Based Screening of the Bromodomain of ATAD2== | |
| + | <StructureSection load='4tz2' size='340' side='right'caption='[[4tz2]], [[Resolution|resolution]] 1.70Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4tz2]] 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=4TZ2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4TZ2 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]] 1.7Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=39R:3-(5-PHENYL-4H-1,2,4-TRIAZOL-3-YL)ANILINE'>39R</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=CSO:S-HYDROXYCYSTEINE'>CSO</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=TRS:2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL'>TRS</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=4tz2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4tz2 OCA], [https://pdbe.org/4tz2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4tz2 RCSB], [https://www.ebi.ac.uk/pdbsum/4tz2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4tz2 ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == 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;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Cellular 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<ref>PMID:25314628</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| + | </div> | ||
| + | <div class="pdbe-citations 4tz2" style="background-color:#fffaf0;"></div> | ||
| + | |||
| + | ==See Also== | ||
| + | *[[ATPase family AAA domain-containing protein|ATPase family AAA domain-containing protein]] | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Chauder BA]] | ||
| + | [[Category: Fesik SW]] | ||
| + | [[Category: Harner MJ]] | ||
| + | [[Category: Phan J]] | ||
Current revision
Fragment-Based Screening of the Bromodomain of ATAD2
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