5X02

Crystal structure of the FLT3 kinase domain bound to the inhibitor FF-10101

5X02 の概要

• エントリーDOI: 10.2210/pdb5x02/pdb
• 分子名称: Receptor-type tyrosine-protein kinase FLT3, N-[(2S)-1-[5-[2-[(4-cyanophenyl)amino]-4-(propylamino)pyrimidin-5-yl]pent-4-ynylamino]-1-oxidanylidene-propan-2-yl]-4-(dimethylamino)-N-methyl-but-2-enamide, SULFATE ION, ... (4 entities in total)
• 機能のキーワード: tyrosine kinase, transferase, irreversible inhibitor complex, kinase catalytic domain, transferase-transferase inihibitor complex, transferase/transferase inihibitor
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 40829.40

構造登録者

Fujikawa, N.,Hirano, D.,Takasaki, M.,Terada, D.,Hagiwara, S.,Park, S.-Y.,Sugiyama, K. (登録日: 2017-01-19, 公開日: 2018-01-24, 最終更新日: 2023-11-22)

• 主引用文献: Yamaura, T.,Nakatani, T.,Uda, K.,Ogura, H.,Shin, W.,Kurokawa, N.,Saito, K.,Fujikawa, N.,Date, T.,Takasaki, M.,Terada, D.,Hirai, A.,Akashi, A.,Chen, F.,Adachi, Y.,Ishikawa, Y.,Hayakawa, F.,Hagiwara, S.,Naoe, T.,Kiyoi, H.; A novel irreversible FLT3 inhibitor, FF-10101, shows excellent efficacy against AML cells withFLT3mutations.; Blood, 131:426-438, 2018; PubMed: 29187377; DOI: 10.1182/blood-2017-05-786657

実験手法

X-RAY DIFFRACTION (2.401 Å)