7U99

EGFR kinase in complex with a macrocyclic inhibitor

7U99 の概要

• エントリーDOI: 10.2210/pdb7u99/pdb
• 分子名称: Epidermal growth factor receptor, 19-chloro-22-methoxy-8,9,11,12,14,15-hexahydro-21H-4,6-ethenopyrimido[5,4-m][1,4,7,10,15]benzotetraoxazacycloheptadecine, CITRATE ANION, ... (4 entities in total)
• 機能のキーワード: egfr, kinase, macrocycle, 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: 1
• 化学式量合計: 38257.41

構造登録者

Beyett, T.S.,Eck, M.J. (登録日: 2022-03-10, 公開日: 2022-11-23, 最終更新日: 2023-10-25)

• 主引用文献: Amrhein, J.A.,Beyett, T.S.,Feng, W.W.,Kramer, A.,Weckesser, J.,Schaeffner, I.K.,Rana, J.K.,Janne, P.A.,Eck, M.J.,Knapp, S.,Hanke, T.; Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.; J.Med.Chem., 65:15679-15697, 2022; PubMed: 36384036; DOI: 10.1021/acs.jmedchem.2c01041

実験手法

X-RAY DIFFRACTION (2.5 Å)