Search

Continuous efforts have been invested in the selective modification of proteins. Herein, we first report the construction of sulfonium tethered cyclic peptides via an intramolecular cyclization by an aliphatic halide. This cyclization could enhance the stability and cellular uptake of peptides. Furthermore, the sulfonium center could be recognized by cysteine in the vicinity of the protein–peptide interacting interface and form a peptide–protein conjugate. [ABSTRACT FROM AUTHOR]

Peptides that induced autophagy at micromolar concentrations with improved proteolytic resistance properties were generated using the facile methionine bis-alkylation method. Notably, a short bicyclic peptide 7f was proven to be the most potent one among the designed peptides in regards to autophagy inducing activity. This study facilitated the development of a peptide-based autophagy inducer and demonstrated the potential applications of the methionine alkylation-based macrocyclization method for the diversity-oriented generation of peptide-based autophagy inducers. [ABSTRACT FROM AUTHOR]