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

doi:10.1039/C9CC02052G

Characterization of FGF401 as a reversible covalent inhibitor of fibroblast growth factor receptor 4†

Zhan Zhou,^a Xiaojuan Chen,^a Ying Fu,^a Ye Zhang,^a Shuyan Dai,^a Jun Li,^a Lin Chen,^b Guangyu Xu,^c Zhuchu Chen^a and Yongheng Chen

*^a

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* Corresponding authors

^a NHC Key Laboratory of Cancer Proteomics & Laboratory of Structural Biology, Xiangya Hospital, Central South University, Changsha, Hunan, China
E-mail: yonghenc@163.com

^b Molecular and Computational Biology Program, Department of Biological Sciences and Department of Chemistry, University of Southern California, Los Angeles, California 90089, USA

^c Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research (Ministry of Education), College of Chemistry and Chemical Engineering, Hunan Normal University, Changsha 410081, China

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.

Chemical Communications

Characterization of FGF401 as a reversible covalent inhibitor of fibroblast growth factor receptor 4†

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

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