Article
Design, synthesis and antitumor activity of a novel FGFR2-selective degrader to overcome resistance of the FGFR2V564F gatekeeper mutation based on a pan-FGFR inhibitor.
European journal of medicinal chemistry - 5 Sept 2024
Hu Zuli, Zhang Qiangsheng, Li Zulong, Yang Hongling, Chen Xin, Zhang Qi, Yang Tianqiong, He Xiaojie, Feng Qiang, He Jun, Yu Luoting
Abstract excerpt
Aberrant activation of fibroblast growth factor receptors (FGFRs) contributes to the development and progression of multiple types of cancer. Although many FGFR inhibitors have been approved by the FDA, their long-term therapeutic efficacy is hampered by acquired resistance to gatekeeper mutations and low subtype selectivity. FGFR2 has been found to be frequently amplified or mutated in many tumors. In this...
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