PMID: 25730907Mar 3, 2015Paper

Inhibition of non-small cell lung cancer (NSCLC) growth by a novel small molecular inhibitor of EGFR

Oncotarget
Jinsong LiJianru Xiao

Abstract

The epidermal growth factor receptor (EGFR) is a therapeutic target (oncotarget) in NSCLC. Using in vitro EGFR kinase activity system, we identified a novel small molecule, WB-308, as an inhibitor of EGFR. WB-308 decreased NSCLC cell proliferation and colony formation, by causing G2/M arrest and apoptosis. Furthermore, WB-308 inhibited the engraft tumor growths in two animal models in vivo (lung orthotopic transplantation model and patient-derived engraft mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 protein. WB-308 was less cytotoxic than Gefitinib. Our study suggests that WB-308 is a novel EGFR-TKI and may be considered to substitute for Gefitinib in clinical therapy for NSCLC.

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Oct 21, 2016·The Journal of Biological Chemistry·Sisi LiuXin-Hua Feng
Aug 21, 2019·International Journal of Molecular Sciences·Keisuke BabaHodaka Fujii
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