5NW2

pVHL:EloB:EloC in complex with (2S,4R)-1-((S)-3,3-dimethyl-2-(oxetane-3-carboxamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (ligand 19)

5NW2 の概要

• エントリーDOI: 10.2210/pdb5nw2/pdb
• 分子名称: Elongin-B, Elongin-C, Von Hippel-Lindau disease tumor suppressor, ... (5 entities in total)
• 機能のキーワード: protein complex, ubiquitin ligase, hypoxia inducible factor, ligase
• 由来する生物種: Homo sapiens (Human); 詳細
• 細胞内の位置: Nucleus : Q15370 Q15369; Isoform 1: Cytoplasm. Isoform 3: Cytoplasm: P40337
• タンパク質・核酸の鎖数: 12
• 化学式量合計: 169007.59

構造登録者

Gadd, M.S.,Soares, P.,Ciulli, A. (登録日: 2017-05-04, 公開日: 2017-09-20, 最終更新日: 2024-01-17)

• 主引用文献: Soares, P.,Gadd, M.S.,Frost, J.,Galdeano, C.,Ellis, L.,Epemolu, O.,Rocha, S.,Read, K.D.,Ciulli, A.; Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298).; J. Med. Chem., 61:599-618, 2018; PubMed: 28853884; DOI: 10.1021/acs.jmedchem.7b00675

実験手法

X-RAY DIFFRACTION (2.2 Å)