5d7x
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal structure of the human BRPF1 bromodomain in complex with XZ08== | |
| + | <StructureSection load='5d7x' size='340' side='right'caption='[[5d7x]], [[Resolution|resolution]] 1.35Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5d7x]] 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=5D7X OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5D7X 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]] 1.35Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NO3:NITRATE+ION'>NO3</scene>, <scene name='pdbligand=XZ8:4-(1-ACETYL-1H-INDOL-3-YL)-5-METHYL-1,2-DIHYDRO-3H-PYRAZOL-3-ONE'>XZ8</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=5d7x FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5d7x OCA], [https://pdbe.org/5d7x PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5d7x RCSB], [https://www.ebi.ac.uk/pdbsum/5d7x PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5d7x ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/BRPF1_HUMAN BRPF1_HUMAN] Component of the MOZ/MORF complex which has a histone H3 acetyltransferase activity. Positively regulates the transcription of RUNX1 and RUNX2.<ref>PMID:16387653</ref> <ref>PMID:18794358</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Small-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<ref>PMID:26982797</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: | + | <div class="pdbe-citations 5d7x" style="background-color:#fffaf0;"></div> |
| - | [[Category: Caflisch | + | |
| + | ==See Also== | ||
| + | *[[Peregrin|Peregrin]] | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Caflisch A]] | ||
| + | [[Category: Zhu J]] | ||
Current revision
Crystal structure of the human BRPF1 bromodomain in complex with XZ08
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