Stapled peptides have received widespread attention in therapeutics due to the superior membrane penetration and in vivo stability. We have developed a series of methods including CIH, TD coupling, Met-Met, and Cys-Met bis-alkylation strategy to switch peptides' secondary structure and enhance their stability and cellular uptake. Here we focus on the peptide macrocyclization method of Met-Met and Cys-Met bis-alkylation strategy to generate more stable and permeable sulfonium-tethered peptides to avoid tedious synthesis, which can be utilized for drug delivery and further broad biological applications.
Keywords: Reversible modification; Stapled peptide; Sulfonium.
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