4G34

Crystal Structure of GSK6924 Bound to PERK (R587-R1092, delete A660-T867) at 2.70 A Resolution

4G34 の概要

• エントリーDOI: 10.2210/pdb4g34/pdb
• 関連するPDBエントリー: 3QD2 4G31
• 分子名称: Eukaryotic translation initiation factor 2-alpha kinase 3, 1-[5-(4-aminothieno[3,2-c]pyridin-3-yl)-2,3-dihydro-1H-indol-1-yl]-2-phenylethanone (3 entities in total)
• 機能のキーワード: deletion mutant, catalytic domain, synthetic inhibitor, 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: 35182.70

構造登録者

Gampe, R.T.,Axten, J.M. (登録日: 2012-07-13, 公開日: 2012-08-08, 最終更新日: 2023-09-13)

• 主引用文献: Axten, J.M.,Medina, J.R.,Feng, Y.,Shu, A.,Romeril, S.P.,Grant, S.W.,Li, W.H.,Heerding, D.A.,Minthorn, E.,Mencken, T.,Atkins, C.,Liu, Q.,Rabindran, S.,Kumar, R.,Hong, X.,Goetz, A.,Stanley, T.,Taylor, J.D.,Sigethy, S.D.,Tomberlin, G.H.,Hassell, A.M.,Kahler, K.M.,Shewchuk, L.M.,Gampe, R.T.; Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK).; J.Med.Chem., 55:7193-7207, 2012; PubMed: 22827572; DOI: 10.1021/jm300713s

実験手法

X-RAY DIFFRACTION (2.7 Å)