6d9x
From Proteopedia
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- | '''Unreleased structure''' | ||
- | + | ==Discovery of Potent 2-Aryl-6,7-Dihydro-5HPyrrolo[ 1,2-a]imidazoles as WDR5 WIN-site Inhibitors Using Fragment-Based Methods and Structure-Based Design== | |
- | + | <StructureSection load='6d9x' size='340' side='right' caption='[[6d9x]], [[Resolution|resolution]] 1.83Å' scene=''> | |
- | + | == Structural highlights == | |
- | + | <table><tr><td colspan='2'>[[6d9x]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D9X OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D9X FirstGlance]. <br> | |
- | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=FZM:2-phenyl-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole'>FZM</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr> | |
- | [[Category: | + | <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=6d9x FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d9x OCA], [http://pdbe.org/6d9x PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d9x RCSB], [http://www.ebi.ac.uk/pdbsum/6d9x PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d9x ProSAT]</span></td></tr> |
+ | </table> | ||
+ | == Function == | ||
+ | [[http://www.uniprot.org/uniprot/WDR5_HUMAN WDR5_HUMAN]] Contributes to histone modification. May position the N-terminus of histone H3 for efficient trimethylation at 'Lys-4'. As part of the MLL1/MLL complex it is involved in methylation and dimethylation at 'Lys-4' of histone H3. H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation. As part of the NSL complex it may be involved in acetylation of nucleosomal histone H4 on several lysine residues. May regulate osteoblasts differentiation.<ref>PMID:19556245</ref> <ref>PMID:19103755</ref> <ref>PMID:20018852</ref> <ref>PMID:16600877</ref> <ref>PMID:16829960</ref> | ||
+ | == References == | ||
+ | <references/> | ||
+ | __TOC__ | ||
+ | </StructureSection> | ||
+ | [[Category: Fesik, S W]] | ||
[[Category: Phan, J]] | [[Category: Phan, J]] | ||
- | [[Category: | + | [[Category: Dna binding protein]] |
+ | [[Category: Dna binding protein-inhibitor complex]] | ||
+ | [[Category: Fragment screening]] | ||
+ | [[Category: Mixed-lineage leukemia]] | ||
+ | [[Category: Structure-based design]] | ||
+ | [[Category: Wdr5]] | ||
+ | [[Category: Win-site]] |
Revision as of 10:07, 5 September 2018
Discovery of Potent 2-Aryl-6,7-Dihydro-5HPyrrolo[ 1,2-a]imidazoles as WDR5 WIN-site Inhibitors Using Fragment-Based Methods and Structure-Based Design
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