6V9C

Crystal structure of FGFR4 kinase domain in complex with covalent inhibitor

6V9C の概要

• エントリーDOI: 10.2210/pdb6v9c/pdb
• 分子名称: Fibroblast growth factor receptor 4, N-[(3R,4S)-4-{[6-(2,6-dichloro-3,5-dimethoxyphenyl)-8-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}oxolan-3-yl]prop-2-enamide, SULFATE ION, ... (4 entities in total)
• 機能のキーワード: tyrosine kinase inhibitor, covalent inhibitor, fgfr, kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 34579.70

構造登録者

Liu, J.,Liu, H. (登録日: 2019-12-13, 公開日: 2020-03-25, 最終更新日: 2023-10-11)

• 主引用文献: Liu, H.,Niu, D.,Tham Sjin, R.T.,Dubrovskiy, A.,Zhu, Z.,McDonald, J.J.,Fahnoe, K.,Wang, Z.,Munson, M.,Scholte, A.,Barrague, M.,Fitzgerald, M.,Liu, J.,Kothe, M.,Sun, F.,Murtie, J.,Ge, J.,Rocnik, J.,Harvey, D.,Ospina, B.,Perron, K.,Zheng, G.,Shehu, E.,D'Agostino, L.A.; Discovery of Selective, Covalent FGFR4 Inhibitors with Antitumor Activity in Models of Hepatocellular Carcinoma.; Acs Med.Chem.Lett., 11:1899-1904, 2020; PubMed: 33062171; DOI: 10.1021/acsmedchemlett.9b00601

実験手法

X-RAY DIFFRACTION (1.9 Å)