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Article

Design, Synthesis, and Biological Evaluation of Dual Inhibitors of EGFRL858R/T790M/ACK1 to Overcome Osimertinib Resistance in Nonsmall Cell Lung Cancers.

Journal of medicinal chemistry - 22 Feb 2024

Wang Aoxue, Shuai Wen, Wu Chengyong, Pei Junping, Yang Panpan, Wang Xin, Li Shutong, Liu Jiaxi, Wang Yuxi, Wang Guan, Ouyang Liang

Abstract excerpt

Activation of the alternative pathways and abnormal signaling transduction are frequently observed in third-generation EGFR-TKIs (epidermal growth factor receptor tyrosine kinase inhibitors)-resistant patients. Wherein, hyperphosphorylation of ACK1 contributes to EGFR-TKIs acquired resistance. Dual inhibition of EGFRL858R/T790M and ACK1 might improve therapeutic efficacy and overcome resistance in lung cancers...

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Identifiers

PMID: 38323982
DOI: 10.1021/acs.jmedchem.3c01934

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