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 blog highlighting recent publications in the area of covalent modification of proteins, particularly relating to covalent-modifier drugs. @CovalentMod on Twitter, @covalentmod@mstdn.science on Mastodon, and @covalentmod.bsky.social on BlueSky
Sulfinyl Aziridines as Stereoselective Covalent Destabilizing Degraders of the Oncogenic Transcription Factor MYC
H. T. Rosen , K. Li , C. E. Stieger , E. L. Li , B. Currier , S. M. Brittain , F. J. Garcia , D. C. Beard , M. D. Jones , S. Haenni...
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Design, synthesis and biological evaluation of the activity-based probes for FGFR covalent inhibitorDandan Zhu, Zijian Zheng, Huixin Huang, Xiaojuan Chen, Shuhong Zhang, Zhuchu Chen, Ting Liu, Guangyu Xu, Ying Fu, Yongheng Chen, European Jo...
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DOI Ansgar Oberheide, Maxime van den Oetelaar, Jakob Scheele, Jan Borggräfe, Semmy Engelen, Michael Sattler, Christian Ottmann, ...
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Nafizul Haque Kazi, Nikolas Klink, Kai Gallant, Gian-Marvin Kipka & Malte Gersch Nat Struct Mol Biol , 2025 https://doi.org/10.1038/s415...