Development of pH-responsive crosslinked peptides that form stable α-helices under weakly acidic conditions

Abstract α-Helical structures in protein surface are frequently related to protein–protein interactions that play important roles in signal transduction. We have developed various crosslinking agents that stabilize the α-helical structure of short peptides. In this article, we report pH-responsive crosslinked peptides that promote helical conformation of the peptides under weakly acidic conditions. We incorporated critical sequence of a synthetic estrogen receptor activity-regulating peptide into our pH-responsive crosslinked peptide. The pH control could provide total structural regulation of the target peptide.