4nr9: Difference between revisions
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==Crystal Structure of the bromodomain of human BAZ2B in complex with acetylated lysine== | ==Crystal Structure of the bromodomain of human BAZ2B in complex with acetylated lysine== | ||
<StructureSection load='4nr9' size='340' side='right' caption='[[4nr9]], [[Resolution|resolution]] 1.98Å' scene=''> | <StructureSection load='4nr9' size='340' side='right' caption='[[4nr9]], [[Resolution|resolution]] 1.98Å' scene=''> | ||
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4nra|4nra]], [[4nrb|4nrb]], [[4nrc|4nrc]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4nra|4nra]], [[4nrb|4nrb]], [[4nrc|4nrc]]</td></tr> | ||
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">BAZ2B, KIAA1476 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">BAZ2B, KIAA1476 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=4nr9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4nr9 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4nr9 RCSB], [http://www.ebi.ac.uk/pdbsum/4nr9 PDBsum]</span></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=4nr9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4nr9 OCA], [http://pdbe.org/4nr9 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4nr9 RCSB], [http://www.ebi.ac.uk/pdbsum/4nr9 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4nr9 ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
<div class="pdbe-citations 4nr9" style="background-color:#fffaf0;"></div> | |||
== References == | == References == | ||
<references/> | <references/> | ||
Revision as of 02:36, 5 August 2016
Crystal Structure of the bromodomain of human BAZ2B in complex with acetylated lysineCrystal Structure of the bromodomain of human BAZ2B in complex with acetylated lysine
Structural highlights
Function[BAZ2B_HUMAN] May play a role in transcriptional regulation interacting with ISWI. Publication Abstract from PubMedBromodomains are epigenetic reader domains that have recently become popular targets. In contrast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylogenetic tree have shallower pockets. We describe successful targeting of the challenging BAZ2B bromodomain using biophysical fragment screening and structure-based optimization of high ligand-efficiency fragments into a novel series of low-micromolar inhibitors. Our results provide attractive leads for development of BAZ2B chemical probes and indicate the whole family may be tractable. Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.,Ferguson FM, Fedorov O, Chaikuad A, Philpott M, Muniz JR, Felletar I, von Delft F, Heightman T, Knapp S, Abell C, Ciulli A J Med Chem. 2013 Dec 27;56(24):10183-7. doi: 10.1021/jm401582c. Epub 2013 Dec 13. PMID:24304323[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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