5e74: Difference between revisions
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<StructureSection load='5e74' size='340' side='right'caption='[[5e74]], [[Resolution|resolution]] 1.78Å' scene=''> | <StructureSection load='5e74' size='340' side='right'caption='[[5e74]], [[Resolution|resolution]] 1.78Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[5e74]] is a 1 chain structure with sequence from [ | <table><tr><td colspan='2'>[[5e74]] 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=5E74 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5E74 FirstGlance]. <br> | ||
</td></tr><tr id=' | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.783Å</td></tr> | ||
<tr id=' | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=5KH:N-(1-ACETYL-1H-INDOL-3-YL)-N-(5-HYDROXY-2-METHYLPHENYL)-3-(TRIFLUOROMETHYL)BENZAMIDE'>5KH</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=5e74 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5e74 OCA], [https://pdbe.org/5e74 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5e74 RCSB], [https://www.ebi.ac.uk/pdbsum/5e74 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5e74 ProSAT]</span></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | |||
</table> | </table> | ||
== Function == | == 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;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Homo sapiens]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
[[Category: Caflisch | [[Category: Caflisch A]] | ||
[[Category: Dolbois | [[Category: Dolbois A]] | ||
[[Category: Lolli | [[Category: Lolli G]] | ||
[[Category: Nevado | [[Category: Nevado C]] | ||
[[Category: Spiliotopoulos | [[Category: Spiliotopoulos D]] | ||
Latest revision as of 09:15, 5 July 2023
Crystal Structure of BAZ2B bromodomain in complex with acetylindole compound UZH50Crystal Structure of BAZ2B bromodomain in complex with acetylindole compound UZH50
Structural highlights
FunctionBAZ2B_HUMAN May play a role in transcriptional regulation interacting with ISWI. Publication Abstract from PubMedSmall-molecule hits for the bromodomains of CREBBP and BAZ2B have been identified by scaffold hopping followed by docking of a set of approximately 200 compounds containing the acetyl indole scaffold. Chemical synthesis of nearly 30 derivatives has resulted in ligands of representatives of three subfamilies of human bromodomains with favorable ligand efficiency. The X-ray crystal structures of three different bromodomains (CREBBP, BAZ2B, and BRPF1b) in complex with acetyl indole derivatives reveal the influence of the gatekeeper residue on the orientation of small-molecule ligands in the acetyl lysine binding site. The "Gatekeeper" Residue Influences the Mode of Binding of Acetyl Indoles to Bromodomains.,Unzue A, Zhao H, Lolli G, Dong J, Zhu J, Zechner M, Dolbois A, Caflisch A, Nevado C J Med Chem. 2016 Apr 14;59(7):3087-97. doi: 10.1021/acs.jmedchem.5b01757. Epub, 2016 Mar 30. PMID:26982797[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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