4QQ5
Crystal Structure of FGF Receptor (FGFR) 4 Kinase Harboring the V550L Gate-Keeper Mutation in Complex With FIIN-2, an Irreversible Tyrosine Kinase Inhibitor Capable of Overcoming FGFR Kinase Gate-Keeper Mutations
4QQ5 の概要
エントリーDOI | 10.2210/pdb4qq5/pdb |
関連するPDBエントリー | 4QQC 4QQJ 4QQT 4QRC |
分子名称 | Fibroblast growth factor receptor 4, N-(4-{[3-(3,5-dimethoxyphenyl)-7-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl]methyl}phenyl)propanamide (2 entities in total) |
機能のキーワード | kinase domain fold, cell signaling, phosphotransferase, plasmamembrane, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
由来する生物種 | Homo sapiens (human) |
細胞内の位置 | Cell membrane; Single-pass type I membrane protein. Isoform 2: Secreted. Isoform 3: Cytoplasm : P22455 |
タンパク質・核酸の鎖数 | 1 |
化学式量合計 | 36810.34 |
構造登録者 | |
主引用文献 | Huang, Z.,Tan, L.,Wang, H.,Liu, Y.,Blais, S.,Deng, J.,Neubert, T.A.,Gray, N.S.,Li, X.,Mohammadi, M. DFG-out Mode of Inhibition by an Irreversible Type-1 Inhibitor Capable of Overcoming Gate-Keeper Mutations in FGF Receptors. Acs Chem.Biol., 10:299-309, 2015 Cited by PubMed: 25317566DOI: 10.1021/cb500674s 主引用文献が同じPDBエントリー |
実験手法 | X-RAY DIFFRACTION (2.203 Å) |
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