4nrb: Difference between revisions
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== Structural highlights == | == Structural highlights == | ||
<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> | <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> | ||
</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>< | </td></tr><tr id='ligand'><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></td></tr> | ||
<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4nr9|4nr9]], [[4nra|4nra]], [[4nrc|4nrc]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4nr9|4nr9]], [[4nra|4nra]], [[4nrc|4nrc]]</td></tr> | ||
<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> | <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><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> | <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=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> | ||
<table> | </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;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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</StructureSection> | </StructureSection> | ||
[[Category: Human]] | [[Category: Human]] | ||
[[Category: Arrowsmith, C H | [[Category: Arrowsmith, C H]] | ||
[[Category: Bountra, C | [[Category: Bountra, C]] | ||
[[Category: Chaikuad, A | [[Category: Chaikuad, A]] | ||
[[Category: Ciulli, A | [[Category: Ciulli, A]] | ||
[[Category: Delft, F von | [[Category: Delft, F von]] | ||
[[Category: Edwards, A M | [[Category: Edwards, A M]] | ||
[[Category: Fedorov, O | [[Category: Fedorov, O]] | ||
[[Category: Felletar, I | [[Category: Felletar, I]] | ||
[[Category: Ferguson, F M | [[Category: Ferguson, F M]] | ||
[[Category: Filippakopoulos, P | [[Category: Filippakopoulos, P]] | ||
[[Category: Knapp, S | [[Category: Knapp, S]] | ||
[[Category: Muniz, J R.C | [[Category: Muniz, J R.C]] | ||
[[Category: | [[Category: Structural genomic]] | ||
[[Category: Acetylated lysine binding protein]] | [[Category: Acetylated lysine binding protein]] | ||
[[Category: Bromodomain]] | [[Category: Bromodomain]] | ||
[[Category: Kiaa1476]] | [[Category: Kiaa1476]] | ||
[[Category: Sgc]] | [[Category: Sgc]] | ||
[[Category: Transcription]] | [[Category: Transcription]] | ||
[[Category: Walp4]] | [[Category: Walp4]] | ||
Revision as of 02:13, 25 December 2014
Crystal Structure of the bromodomain of human BAZ2B in complex with compound-1 N01197Crystal Structure of the bromodomain of human BAZ2B in complex with compound-1 N01197
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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