8W9B

CryoEM structure of human PI3K-alpha (P85/P110-H1047R) with QR-8557 binding at an allosteric site

8W9B の概要

• エントリーDOI: 10.2210/pdb8w9b/pdb
• EMDBエントリー: 37363
• 分子名称: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, Phosphatidylinositol 3-kinase regulatory subunit alpha, 1-[(1S)-1-(5-fluoranyl-3-methyl-1-benzofuran-2-yl)-2-methyl-propyl]-3-(1-oxidanylidene-2,3-dihydroisoindol-5-yl)urea (3 entities in total)
• 機能のキーワード: pi3k-alpha, lipid kinase, allosteric inhibition, oncoprotein
• 由来する生物種: Homo sapiens (human); 詳細
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 158293.14

構造登録者

Huang, X.,Ren, X.,Zhong, W. (登録日: 2023-09-05, 公開日: 2024-04-17, 最終更新日: 2024-05-08)

• 主引用文献: Huang, X.,Wang, K.,Han, J.,Chen, X.,Wang, Z.,Wu, T.,Yu, B.,Zhao, F.,Wang, X.,Li, H.,Xie, Z.,Zhu, X.,Zhong, W.,Ren, X.; Cryo-EM structures reveal two allosteric inhibition modes of PI3K alpha H1047R involving a re-shaping of the activation loop.; Structure, 2024; PubMed: 38582077; DOI: 10.1016/j.str.2024.03.007

実験手法

ELECTRON MICROSCOPY (3 Å)