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Characterization of FGF401 as a reversible covalent inhibitor of fibroblast growth factor receptor 4†
Zhan Zhou,Xiaojuan Chen,Ying Fu,Ye Zhang,Shuyan Dai,Jun Li,Lin Chen,Guangyu Xu,Zhuchu Chen,Yongheng Chen
Chemical Communications Pub Date : 04/26/2019 00:00:00 , DOI:10.1039/C9CC02052G
Abstract

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.

Graphical abstract: Characterization of FGF401 as a reversible covalent inhibitor of fibroblast growth factor receptor 4
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