Article
Discovery of a Selective and Orally Bioavailable FGFR2 Degrader for Treating Gastric Cancer.
Journal of medicinal chemistry - 8 Jun 2023
Ma Lin, Li Yingying, Luo Ruixiang, Wang Yuhan, Cao Jiaqi, Fu Weitao, Qian Bolan, Zheng Lei, Tang Longguang, Lv Xinting, Zheng Lulu, Liang Guang, Chen Lingfeng
Abstract excerpt
Abnormal activation of fibroblast growth factor receptors (FGFRs) results in the development and progression of human cancers. FGFR2 is frequently amplified or mutated in cancers; therefore, it is an attractive target for tumor therapy. Despite the development of several pan-FGFR inhibitors, their long-term therapeutic efficacy is hindered by acquired mutations and low isoform selectivity. Herein, we report the...
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