7LG8

EGFR (T79M/V948R) in complex with naquotinib and an allosteric inhibitor

Summary for 7LG8

• Entry DOI: 10.2210/pdb7lg8/pdb
• Descriptor: 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, 6-ethyl-3-[[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]amino]-5-[(3R)-1-prop-2-enoylpyrrolidin-3-yl]oxy-pyrazin e-2-carboxamide, ... (4 entities in total)
• Functional Keywords: egfr, kinase, inhibitor, allosteric, transferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 4
• Total formula weight: 155375.82

Authors

Beyett, T.S.,Eck, M.J. (deposition date: 2021-01-19, release date: 2022-02-23, Last modification date: 2023-10-18)

• Primary citation: 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, 13:2530-2530, 2022; PubMed: 35534503; DOI: 10.1038/s41467-022-30258-y

Experimental method

X-RAY DIFFRACTION (2.93 Å)