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Published on: September 28, 2022
An intramolecular tryptophan-condensation approach for peptide stapling
Eunice Y-L Hui1, Bhimsen Rout, Yaw Sing Tan
1Division of Organic Chemistry, Institute of Chemical and Engineering Sciences, Agency for Science Technology and Research (A*STAR), Singapore 138665. eunicehui@ices.a-star.edu.sg charles_johannes@ices.a-star.edu.sg.
Abstract:
Stapled peptides are gaining tremendous interest as next-generation therapeutic agents to target protein-protein interactions. Herein, we report an intramolecular peptide stapling method which links two tryptophan residues at the C2 position of the indole moieties via acid-mediated condensation with an aldehyde.
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