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.
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Site-Specific Molecular Glues for the 14-3-3/Tau pS214 ProteinProtein Interaction via Reversible Covalent Imine Tethering

DOI Ansgar Oberheide,   Maxime van den Oetelaar,   Jakob Scheele,   Jan Borggräfe,   Semmy Engelen,   Michael Sattler,   Christian Ottmann, ...