Tuesday, April 30, 2019

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  and  Yongheng Chen

Chem. Commun., 2019

DOI: 10.1039/C9CC02052G

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.

A practical method for determining the rate of covalent modification of fragments and leads

Janice Jeon, Svetlana A. Kholodar, Brian H. Tran, Kimberly E. Mallinger, Daniel A. Erlanson & Robert A. Everley  Nat Commun   16 , 11234...