Article
Optimization of Aminoindazole derivatives as highly selective covalent inhibitors for wild-type and mutant FGFR4.
Bioorganic chemistry - 15 Jun 2025
Guo Jing, Chen Xiaojuan, Li Xiaofei, Wang Xuan, Shao Min, Song Xiaojuan, Zhang Lin, Huang Shengjie, Patterson Adam V, Smaill Jeff B, Zhou Yang, Yu Xiangrong, Chen Yongheng, Lu Xiaoyun
Abstract excerpt
The Fibroblast growth factor receptor 4 (FGFR4) has emerged as a potential oncogenic driver in hepatocellular carcinoma (HCC), primarily due to aberrations in the FGFR4-FGF19 signaling axis. Although the FGFR4-selective inhibitors have been reported, none have received approval. Further, the clinical acquired resistance caused by FGFR4 mutations has become an unmet clinical need for cancer therapy. In this study,...
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