7LGS

Structure of EGFR_D770_N771insNPG/V948R in complex with covalent inhibitor Osimertinib.

Summary for 7LGS

• Entry DOI: 10.2210/pdb7lgs/pdb
• Descriptor: Epidermal growth factor receptor, ~{N}-[2-[2-(dimethylamino)ethyl-methyl-amino]-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]propanamide, 1,2-ETHANEDIOL, ... (5 entities in total)
• Functional Keywords: kinase, inhibitor, covalent, hydrolase, hydrolase-hydrolase inhibitor complex, hydrolase/hydrolase inhibitor
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 4
• Total formula weight: 153321.10

Authors

Skene, R.J.,Lane, W. (deposition date: 2021-01-21, release date: 2021-09-22, Last modification date: 2023-10-18)

• Primary citation: Gonzalvez, F.,Vincent, S.,Baker, T.E.,Gould, A.E.,Li, S.,Wardwell, S.D.,Nadworny, S.,Ning, Y.,Zhang, S.,Huang, W.S.,Hu, Y.,Li, F.,Greenfield, M.T.,Zech, S.G.,Das, B.,Narasimhan, N.I.,Clackson, T.,Dalgarno, D.,Shakespeare, W.C.,Fitzgerald, M.,Chouitar, J.,Griffin, R.J.,Liu, S.,Wong, K.K.,Zhu, X.,Rivera, V.M.; Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer.; Cancer Discov, 11:1672-1687, 2021; PubMed: 33632773; DOI: 10.1158/2159-8290.CD-20-1683

Experimental method

X-RAY DIFFRACTION (3.1 Å)