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.

Oncogenic KRAS G12C: Kinetic and Redox Characterization of Covalent Inhibition

Minh V. Huynh, Derek Parsonage, Tom E. Forshaw, Venkat R. Chirasani, G. Aaron Hobbs, Hanzhi Wu, Jingyun Lee, Cristina M. Furdui, Leslie B. P...