Peptide Stapling and Conjugation via Reversible Crosslinking of Two Alkyl Amines Using Formamidine

Keywords

peptide stapling - reversible crosslinking - formamidine - alkyl amines

Significance

Amino groups can be found in numerous natural and synthetic compounds and serve as good sites of accessibility to modify several native bioactive molecules. However, not so many methods have been established for the ligation of two amino groups with reversible linkers for bioconjugation applications. The authors herein report a novel cogent method to achieve this goal using a formamidine linker.

Comment

A variety of stapled peptides and amines were prepared in good yields from their respective primary and secondary amines under the standard conditions with the help of a formamidine linker. The linkage involves hetero-coupling selectivity between the primary and secondary amines to afford the stapled products or bioconjugates of some conventional drugs.

Publikationsverlauf

Artikel online veröffentlicht:
22. April 2025