4M7I

Crystal Structure of GSK6157 Bound to PERK (R587-R1092, delete A660-T867) at 2.34A Resolution

4M7I の概要

• エントリーDOI: 10.2210/pdb4m7i/pdb
• 関連するPDBエントリー: 3QD2 4G31 4G34
• 分子名称: Eukaryotic translation initiation factor 2-alpha kinase 3, 1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-1H-indol-1-yl]-2-(6-methylpyridin-2-yl)ethanone (3 entities in total)
• 機能のキーワード: deletion mutant, catalytic domain, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human); 詳細
• 細胞内の位置: Endoplasmic reticulum membrane; Single-pass type I membrane protein: Q9NZJ5
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 35211.65

構造登録者

Gampe, R.T.,Axten, J.M. (登録日: 2013-08-12, 公開日: 2014-09-03, 最終更新日: 2023-09-20)

• 主引用文献: Axten, J.M.,Romeril, S.P.,Shu, A.,Ralph, J.,Medina, J.R.,Feng, Y.,Li, W.H.H.,Grant, S.W.,Heerding, D.A.,Minthorn, E.,Mencken, T.,Gaul, N.,Goetz, A.,Stanley, T.,Hassell, A.M.,Gampe, R.T.,Atkins, C.,Kumar, R.; Discovery of 5-{4-fluoro-1-[(6-methyl-2-pyridinyl)acetyl]-2,3-dihydro-1H-indol-5-yl}-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2656157), a Potent and Selective PERK Inhibitor Selected for Preclinical Development; To be Published,

実験手法

X-RAY DIFFRACTION (2.34 Å)