Article
Lamellarin 14, a derivative of marine alkaloids, inhibits the T790M/C797S mutant epidermal growth factor receptor.
Cancer science - 1 May 2021
Nishiya Naoyuki, Oku Yusuke, Ishikawa Chie, Fukuda Tsutomu, Dan Shingo, Mashima Tetsuo, Ushijima Masaru, Furukawa Yoko, Sasaki Yuka, Otsu Keishi, Sakyo Tomoko, Abe Masanori, Yonezawa Honami, Ishibashi Fumito, Matsuura Masaaki, Tomida Akihiro, Seimiya Hiroyuki, Yamori Takao, Iwao Masatomo, Uehara Yoshimasa
Abstract excerpt
The emergence of acquired resistance is a major concern associated with molecularly targeted kinase inhibitors. The C797S mutation in the epidermal growth factor receptor (EGFR) confers resistance to osimertinib, a third-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI). We report that the derivatization of the marine alkaloid topoisomerase inhibitor lamellarin N provides a structurally new class of EGFR-TKIs....
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