Journal
CCS CHEMISTRY
Volume 5, Issue 6, Pages 1433-1442Publisher
CHINESE CHEMICAL SOC
DOI: 10.31635/ccschem.022.202201985
Keywords
sulfonium; protein covalent modification; proteolysis targeting chimeras; site-specific modification; degradation
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This article introduces a proximity-triggered group transfer strategy, which enables the transfer of groups from a sulfonium warhead to a Cysteine residue near the binding interface. Successful intracellular transfer of sulfonium 1-X was achieved, leading to the degradation of epidermal growth factor receptors and highlighting the potential of this strategy in chemical biology studies.
Over the past 20 years, great efforts have been invested in developing site-specific approaches to protein modification to dissect protein functions directly and accurately. Here, we report a proximity-triggered group transfer strategy from a sulfonium warhead to a Cysteine (Cys) residue of the target protein. With a guiding ligand, cargoes could be transferred selectively from a sulfonium center onto the Cys residue in the vicinity of their binding interface. The successful thalidomide transfer of sulfonium 1-X could be applied intracellularly for epidermal growth factor receptor degradation, highlighting the potential of group transfer strategy as a suite of chemical biology studies, including cell imaging, protein profiling, and protein degradation by simply employing different transferrable groups. [GRAPHICS] .
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