American journal of respiratory and critical care medicine
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Am. J. Respir. Crit. Care Med. · Apr 2016
Small-molecule, T315, Promotes CBL-dependent Degradation of EGFR via Y1045 Autophosphorylation.
Despite the fact that tyrosine kinase inhibitors (TKIs) have been found effective in treating patients harboring activating mutations of epidermal growth factor receptor (EGFR), an acquired secondary mutation, T790M, which lowers the affinity to TKIs, can lead to EGFR TKI resistance after this standard treatment. ⋯ Our evidence suggests that T315 is a novel class of anticancer drug that is able to inhibit the growth of EGFR-TKI-resistant lung adenocarcinoma cells by inducing the degradation of EGFR.