Discovery of an orally effective double-stapled peptide for reducing ovariectomy-induced bone loss in mice.

ABSTRACT: Stapled peptides with significantly enhanced pharmacological profiles have emerged as promising therapeutic molecules due to their remarkable resistance to proteolysis and performance to penetrate cells. The all-hydrocarbon peptide stapling technique has already widely adopted with great success, yielding numerous potent peptide-based molecules. Based on our prior efforts, we conceived and prepared a double-stapled peptide in this study, termed FRNC-1, which effectively attenuated the bone resorption capacity of mature osteoclasts in vitro through specific inhibition of phosphorylated GSK-3β. The double-stapled peptide FRNC-1 displayed notably improved helical contents and resistance to proteolysis than its linear form. Additionally, FRNC-1 effectively prevented osteoclast ac

SUBMITTER: Cong W 

PROVIDER: S-EPMC10502273 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature