View source for 4nrc


==Crystal Structure of the bromodomain of human BAZ2B in complex with compound-3 N01186==
<StructureSection load='4nrc' size='340' side='right'caption='[[4nrc]], [[Resolution|resolution]] 1.86&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4nrc]] 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=4NRC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4NRC 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]] 1.86&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=15P:POLYETHYLENE+GLYCOL+(N=34)'>15P</scene>, <scene name='pdbligand=2LY:N-METHYL-2,3-DIHYDROTHIENO[3,4-B][1,4]DIOXINE-5-CARBOXAMIDE'>2LY</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=4nrc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4nrc OCA], [https://pdbe.org/4nrc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4nrc RCSB], [https://www.ebi.ac.uk/pdbsum/4nrc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4nrc ProSAT]</span></td></tr>
</table>
== Function ==
[https://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 ==
Bromodomains 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<ref>PMID:24304323</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 4nrc" style="background-color:#fffaf0;"></div>

==See Also==
*[[Bromodomain adjacent to zinc finger 3D structures|Bromodomain adjacent to zinc finger 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Arrowsmith CH]]
[[Category: Bountra C]]
[[Category: Chaikuad A]]
[[Category: Ciulli A]]
[[Category: Edwards AM]]
[[Category: Fedorov O]]
[[Category: Felletar I]]
[[Category: Ferguson FM]]
[[Category: Filippakopoulos P]]
[[Category: Knapp S]]
[[Category: Muniz JRC]]
[[Category: Von Delft F]]