L718Q mutant EGFR escapes covalent inhibition by stabilizing a non-reactive conformation of the lung cancer drug osimertinib

Osimertinib is a third-generation inhibitor approved for the treatment of non-small cell lung cancer. It overcomes resistance to first-generation inhibitors by incorporating an acrylamide group which alkylates Cys797 of EGFR T790M. The mutation of a residue in the P-loop (L718Q) was shown to cause r...

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Detalles Bibliográficos
Autores principales: Callegari, D., Ranaghan, K. E., Woods, C. J., Minari, R., Tiseo, M., Mor, M., Mulholland, A. J., Lodola, A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2018
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5911825/
https://www.ncbi.nlm.nih.gov/pubmed/29732058
http://dx.doi.org/10.1039/c7sc04761d

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