Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5433354 | Journal of Controlled Release | 2017 | 10 Pages |
Artificial cationic helical peptides possess an enhanced cell-penetrating property. However, their cell-penetrability is not converted by cellular environmental changes resulting in nonspecific uptake. In this study, pH-sensitive anion-donating groups were added to a helical polypeptide to simultaneously achieve tumor targeting and pro-apoptotic activity. The mitochondria-destabilizing helical polypeptide undergoing pH-dependent conformational transitions selectively targeted cancer cells consequently disrupting mitochondrial membranes and subsequently inducing apoptosis. This work presents a promising peptide therapeutic system for cancer therapy.
Graphical abstractMitochondria-destabilizing helical polypeptide undergoing a pH-activated conformational transition selectively perturbed the mitochondrial outer membranes thereby inducing pro-apoptosis.Download high-res image (74KB)Download full-size image