Article ID Journal Published Year Pages File Type
5433354 Journal of Controlled Release 2017 10 Pages PDF
Abstract

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

Related Topics
Physical Sciences and Engineering Materials Science Biomaterials
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