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
Lysine-Targeted Covalent Inhibition of eIF4E with an Anionic Electrophile Warhead
Paramita Pal, Erika M. James, Caitlyn E. Given, Hong Yue, Rebecca J. Metivier, Jianwei Che, Eric S. Fischer, Lyn H. Jones; ACS Chem. Biol ....
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Xu-liang Xu, Ti-ti Ying, Xiao-wen Wu, Yun-jun Chen, Gang-ao Hu, Yu-tian Guan, Shi-yi Liu, He Wang, Mohamed Seif, Mahmoud Emam, Hong Wang, We...
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Joseph E Klebba, Nilotpal Roy, Steffen M Bernard, Stephanie Grabow, Melissa A. Hoffman, Hui Miao, Junko Tamiya, Jinwei Wang, Cynthia Berry, ...
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Ran Cheng, Hanfeng Lin, Xin Yu, Shrilekha Misra, Andrew D. Mitchell, Jennifer A. Woyach, Xiaoli Qi & Jin Wang Nat Commun (2026). https:...