8Q1N
Cyclic peptide binder of the WBM-site of WDR5
Summary for 8Q1N
Entry DOI | 10.2210/pdb8q1n/pdb |
Descriptor | WD repeat-containing protein 5, Cyclic peptide inhibitor (3 entities in total) |
Functional Keywords | inhibitor, wd-repeat, gene regulation |
Biological source | Homo sapiens (human) More |
Total number of polymer chains | 4 |
Total formula weight | 73108.64 |
Authors | Schmeing, S.,Chang, J.Y.,t Hart, P.,Gasper, R. (deposition date: 2023-08-01, release date: 2023-09-06, Last modification date: 2023-09-13) |
Primary citation | Chang, J.Y.,Neugebauer, C.,Schmeing, S.,Amrahova, G.,'t Hart, P. Macrocyclic peptides as inhibitors of WDR5-lncRNA interactions. Chem.Commun.(Camb.), 59:10656-10659, 2023 Cited by PubMed Abstract: WDR5 is an adaptor protein involved in the regulation of various epigenetic modifier complexes. Various inhibitors have been described but only as inhibitors of its protein-protein interactions. Here we describe peptidic macrocycles that act as inhibitors of the interaction between WDR5 and long non-coding RNAs. The findings provide a new strategy to modulate the biological function of WDR5 as an RNA binding epigenetic regulator. PubMed: 37581220DOI: 10.1039/d3cc03221c PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.843 Å) |
Structure validation
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