8Q1N

Cyclic peptide binder of the WBM-site of WDR5

8Q1N の概要

• エントリーDOI: 10.2210/pdb8q1n/pdb
• 分子名称: WD repeat-containing protein 5, Cyclic peptide inhibitor (3 entities in total)
• 機能のキーワード: inhibitor, wd-repeat, gene regulation
• 由来する生物種: Homo sapiens (human); 詳細
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 73108.64

構造登録者

Schmeing, S.,Chang, J.Y.,t Hart, P.,Gasper, R. (登録日: 2023-08-01, 公開日: 2023-09-06, 最終更新日: 2024-11-13)

主引用文献

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

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: 37581220
DOI: 10.1039/d3cc03221c

実験手法

X-RAY DIFFRACTION (1.843 Å)