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7U98

EGFR(T790M/V948R) in complex with a macrocyclic inhibitor

Summary for 7U98
Entry DOI10.2210/pdb7u98/pdb
DescriptorEpidermal growth factor receptor, 19-chloro-18-fluoro-22-methoxy-8,9,11,12,14,15-hexahydro-21H-4,6-ethenopyrimido[5,4-m][1,4,7,10,15]benzotetraoxazacycloheptadecine (2 entities in total)
Functional Keywordsegfr, kinase, macrocycle, inhibitor, transferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological sourceHomo sapiens (human)
Total number of polymer chains4
Total formula weight152697.83
Authors
Beyett, T.S.,Eck, M.J. (deposition date: 2022-03-10, release date: 2022-11-23, Last modification date: 2023-10-25)
Primary citationAmrhein, 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
Cited by
PubMed: 36384036
DOI: 10.1021/acs.jmedchem.2c01041
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (3.42 Å)
Structure validation

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