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6e23
From Proteopedia
(Difference between revisions)
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| - | '''Unreleased structure''' | ||
| - | + | ==Displacement of WDR5 from chromatin by a pharmacological WIN site inhibitor with picomolar affinity== | |
| - | + | <StructureSection load='6e23' size='340' side='right'caption='[[6e23]], [[Resolution|resolution]] 1.66Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[6e23]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6E23 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6E23 FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=EPE:4-(2-HYDROXYETHYL)-1-PIPERAZINE+ETHANESULFONIC+ACID'>EPE</scene>, <scene name='pdbligand=HLJ:N-[(3,4-dichlorophenyl)methyl]-3-(6-fluoro-2-methylpyridin-3-yl)-5-{[(2E)-2-imino-3-methyl-2,3-dihydro-1H-imidazol-1-yl]methyl}benzamide'>HLJ</scene></td></tr> | |
| - | [[Category: | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6d9x|6d9x]]</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=6e23 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6e23 OCA], [http://pdbe.org/6e23 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6e23 RCSB], [http://www.ebi.ac.uk/pdbsum/6e23 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6e23 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: Large Structures]] | ||
| + | [[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: Gene regulation]] | ||
| + | [[Category: Gene regulation-inhibitor complex]] | ||
| + | [[Category: Mixed-lineage leukemia]] | ||
| + | [[Category: Structure-based design]] | ||
| + | [[Category: Wdr5]] | ||
| + | [[Category: Win-site]] | ||
Revision as of 11:56, 13 March 2019
Displacement of WDR5 from chromatin by a pharmacological WIN site inhibitor with picomolar affinity
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