4nrb

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{{STRUCTURE_4nrb| PDB=4nrb | SCENE= }}
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==Crystal Structure of the bromodomain of human BAZ2B in complex with compound-1 N01197==
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===Crystal Structure of the bromodomain of human BAZ2B in complex with compound-1 N01197===
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<StructureSection load='4nrb' size='340' side='right' caption='[[4nrb]], [[Resolution|resolution]] 2.08&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4nrb]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4NRB OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4NRB FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2LX:N-METHYL-2-(TETRAHYDRO-2H-PYRAN-4-YLOXY)BENZAMIDE'>2LX</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene><br>
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<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4nr9|4nr9]], [[4nra|4nra]], [[4nrc|4nrc]]</td></tr>
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<tr><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>
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4nrb FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4nrb OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4nrb RCSB], [http://www.ebi.ac.uk/pdbsum/4nrb PDBsum]</span></td></tr>
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<table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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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.
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==Function==
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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>
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[[http://www.uniprot.org/uniprot/BAZ2B_HUMAN BAZ2B_HUMAN]] May play a role in transcriptional regulation interacting with ISWI.
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==About this Structure==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[4nrb]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4NRB OCA].
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</div>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Human]]
[[Category: Arrowsmith, C H.]]
[[Category: Arrowsmith, C H.]]
[[Category: Bountra, C.]]
[[Category: Bountra, C.]]

Revision as of 06:23, 2 July 2014

Crystal Structure of the bromodomain of human BAZ2B in complex with compound-1 N01197

4nrb, resolution 2.08Å

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