6N3L

Identification of novel, potent and selective GCN2 inhibitors as first-in-class anti-tumor agents

6N3L の概要

• エントリーDOI: 10.2210/pdb6n3l/pdb
• 分子名称: eIF-2-alpha kinase GCN2,eIF-2-alpha kinase GCN2, N-{6-[(1-methyl-2-{[4-(trifluoromethyl)phenyl]amino}-1H-benzimidazol-5-yl)oxy]pyrimidin-4-yl}cyclopropanecarboxamide (3 entities in total)
• 機能のキーワード: gcn2, kinase, inhibitor, anti-tumor, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 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: 76638.10

構造登録者

Hoffman, I.D.,Fujimoto, J.,Kurasawa, O.,Takagi, T.,Klein, M.G.,Kefala, G.,Ding, S.C.,Cary, D.R.,Mizojiri, R. (登録日: 2018-11-15, 公開日: 2019-10-09, 最終更新日: 2024-03-13)

• 主引用文献: Fujimoto, J.,Kurasawa, O.,Takagi, T.,Liu, X.,Banno, H.,Kojima, T.,Asano, Y.,Nakamura, A.,Nambu, T.,Hata, A.,Ishii, T.,Sameshima, T.,Debori, Y.,Miyamoto, M.,Klein, M.G.,Tjhen, R.,Sang, B.C.,Levin, I.,Lane, S.W.,Snell, G.P.,Li, K.,Kefala, G.,Hoffman, I.D.,Ding, S.C.,Cary, D.R.,Mizojiri, R.; Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.; Acs Med.Chem.Lett., 10:1498-1503, 2019; PubMed: 31620240; DOI: 10.1021/acsmedchemlett.9b00400

実験手法

X-RAY DIFFRACTION (2.61 Å)