Exceptions to a long-held rule against chemically bonding to biological targets are powering new cancer medicines, finds Andy Extance
https://www.chemistryworld.com/feature/covalent-inhibitor-drugs/2500494.article
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
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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...
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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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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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Nafizul Haque Kazi, Nikolas Klink, Kai Gallant, Gian-Marvin Kipka & Malte Gersch Nat Struct Mol Biol , 2025 https://doi.org/10.1038/s415...