Article
Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2.
Bioorganic & medicinal chemistry - 1 Mar 2023
Cui Yetong, Wang Ruonan, Wei Yujiao, Hou Fei, Li Haixi, Jiang Yurui, Sun Yue, Fu Shushu, Zuo Lina, Wang Xiaoji, Li Ming, Li Jinling, Liu Ning, Zhang Kun, Wei Mingming, Yang Guang
Abstract excerpt
In previous decades, patients with the most active EGFR mutations in non-small cell lung cancer (NSCLC) have significantly benefited from EGFR tyrosine kinase inhibitors (TKIs). However, a minority with EGFR and HER2 exon 20 mutations are inherently resistant to treatment. Several molecular TKIs (such as TAK788 and Poziotinib) were recently discovered and demonstrated as effective inhibitors against the most...
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