Article
Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance.
Journal of medicinal chemistry - 23 Sept 2021
Finlay M Raymond V, Barton Peter, Bickerton Sue, Bista Michal, Colclough Nicola, Cross Darren A E, Evans Laura, Floc'h Nicolas, Gregson Clare, Guérot Carine M, Hargreaves David, Kang Xiaoming, Lenz Eva M, Li Xu, Liu Yi, Lorthioir Olivier, Martin Matthew J, McKerrecher Darren, McWhirter Claire, O'Neill Daniel, Orme Jonathan P, Mosallanejad Arash, Rahi Amar, Smith Paul D, Talbot Verity, Ward Richard A, Wrigley Gail, Wylot Marta, Xue Lin, Yao Tieguang, Ye Yang, Zhao Xiliang
Abstract excerpt
The epidermal growth factor receptor (EGFR) harboring activating mutations is a clinically validated target in non-small-cell lung cancer, and a number of inhibitors of the EGFR tyrosine kinase domain, including osimertinib, have been approved for clinical use. Resistance to these therapies has emerged due to a variety of molecular events including the C797S mutation which renders third-generation C797-targeting...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.