4xua
From Proteopedia
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| - | ''' | + | ==Crystal Structure of the bromodomain of human BAZ2B in complex with E11919 BAZ2-ICR analogue== |
| + | <StructureSection load='4xua' size='340' side='right' caption='[[4xua]], [[Resolution|resolution]] 1.75Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4xua]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4XUA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4XUA FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=43C:4-{1-[2-(4-METHYL-1H-1,2,3-TRIAZOL-1-YL)ETHYL]-4-PHENYL-1H-IMIDAZOL-5-YL}BENZONITRILE'>43C</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'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4xua FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xua OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4xua RCSB], [http://www.ebi.ac.uk/pdbsum/4xua PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/BAZ2B_HUMAN BAZ2B_HUMAN]] May play a role in transcriptional regulation interacting with ISWI. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The bromodomain containing proteins BAZ2A/B play essential roles in chromatin remodeling and regulation of noncoding RNAs. We present the structure based discovery of a potent, selective, and cell active inhibitor 13 (BAZ2-ICR) of the BAZ2A/B bromodomains through rapid optimization of a weakly potent starting point. A key feature of the presented inhibitors is an intramolecular aromatic stacking interaction that efficiently occupies the shallow bromodomain pockets. 13 represents an excellent chemical probe for functional studies of the BAZ2 bromodomains in vitro and in vivo. | ||
| - | + | Structure Enabled Design of BAZ2-ICR, A Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B.,Drouin L, McGrath S, Vidler LR, Chaikuad A, Monteiro O, Tallant C, Philpott M, Rogers C, Fedorov O, Liu M, Akhtar W, Hayes A, Raynaud F, Muller S, Knapp S, Hoelder S J Med Chem. 2015 Feb 26. PMID:25719566<ref>PMID:25719566</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | == References == | |
| - | [[Category: | + | <references/> |
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Arrowsmith, C H]] | ||
| + | [[Category: Bountra, C]] | ||
[[Category: Chaikuad, A]] | [[Category: Chaikuad, A]] | ||
| + | [[Category: Delft, F von]] | ||
| + | [[Category: Edwards, A M]] | ||
| + | [[Category: Felletar, I]] | ||
[[Category: Knapp, S]] | [[Category: Knapp, S]] | ||
| - | [[Category: | + | [[Category: Structural genomic]] |
| - | [[Category: | + | [[Category: Acetylated lysine binding protein]] |
| - | [[Category: | + | [[Category: Bromodomain]] |
| - | [[Category: | + | [[Category: Kiaa1476]] |
| - | [[Category: | + | [[Category: Sgc]] |
| - | [[Category: | + | [[Category: Transcription]] |
| + | [[Category: Walp4]] | ||
Revision as of 11:46, 11 March 2015
Crystal Structure of the bromodomain of human BAZ2B in complex with E11919 BAZ2-ICR analogue
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