7K1H

EGFR L858R/V948R in complex with osimertinib and allosteric inhibitor JBJ-09-063

7K1H の概要

• エントリーDOI: 10.2210/pdb7k1h/pdb
• 分子名称: Epidermal growth factor receptor, (2R)-2-(5-fluoro-2-hydroxyphenyl)-2-{6-[4-(1-methylpiperidin-4-yl)phenyl]-1-oxo-1,3-dihydro-2H-isoindol-2-yl}-N-(1,3-thiazol-2-yl)acetamide, N-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide, ... (4 entities in total)
• 機能のキーワード: egfr, kinase, allosteric, inhibitor, transferase, 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: 6
• 化学式量合計: 232768.78

構造登録者

Beyett, T.S.,Eck, M.J. (登録日: 2020-09-07, 公開日: 2021-09-15, 最終更新日: 2023-10-18)

• 主引用文献: Beyett, T.S.,To, C.,Heppner, D.E.,Rana, J.K.,Schmoker, A.M.,Jang, J.,De Clercq, D.J.H.,Gomez, G.,Scott, D.A.,Gray, N.S.,Janne, P.A.,Eck, M.J.; Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors; Nat Commun, 13:2530-, 2022; DOI: 10.1038/s41467-022-30258-y

実験手法

X-RAY DIFFRACTION (2.602 Å)