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Characterization of FGF401 as a reversible covalent inhibitor of fibroblast growth factor receptor 4
- Zhou, Zhan, Chen, Xiaojuan, Fu, Ying, Zhang, Ye, Dai, Shuyan, Li, Jun, Chen, Lin, Xu, Guangyu, Chen, Zhuchu, Chen, Yongheng
- Chemical communications 2019 v.55 no.42 pp. 5890-5893
- chemical compounds, chemical reactions, fibroblast growth factor receptor 4, mechanism of action, mutation
- Biochemical and structural studies provide information on the mode of action of FGF401 as a selective, reversible covalent inhibitor of FGFR4. Kinase and proliferation assays reveal that FGF401 has the ability to overcome gatekeeper mutations in FGFR4.