We attempted to design a novel cell-based assay for the evaluation of inhibitor efficacy against cancer-related mutations and thus established non-tumorigenic immortalized breast epithelial cells (MCF 10A) whose proliferation depends on epidermal growth factor and which stably overexpress mutant cancer-related genes. Anticancer agents, including molecule-targeted drugs, were evaluated in this assay system to determine their ability to inhibit cell proliferation. As expected, the growth inhibitory activity of molecule-targeted drugs depended on the mutations, similar to their clinical effects. This assay system allows evaluation reflecting the state of cancer tissue in the organism. Furthermore, we suggest that it is also possible to use this assay system for the evaluation of mutant-selective inhibitors and drug screening.
|Normal MCF10A||EGFR L858R-overexpressing MCF10A|
|■: EGFR ■: p-EGFR|
Construction of a Novel Cell-Based Assay for the Evaluation of anti-EGFR Drug Efficacy Against EGFR Mutation. Hoshi H et al. Oncol. Rep. 37 (1), 66-76 (2017).
TAS0728, A Covalent-binding, HER2-selective Kinase Inhibitor Shows Potent Antitumor Activity in Preclinical Models. Irie H, et al. Mol. Cancer Ther. 18 (4), 733-742 (2019).
|Available gene list||Excel|