Conformation-switchable helical polypeptide eliciting selective pro-apoptotic activity for cancer therapy

Publication date: 28 October 2017
Source:Journal of Controlled Release, Volume 264
Author(s): DaeYong Lee, Soo-Hwan Lee, Youjin Na, Ilkoo Noh, JongHoon Ha, Jisang Yoo, Hyun Bae Bang, Jong Hyun Park, Ki Jun Jeong, Chae-Ok Yun, Yeu-Chun Kim
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 abstract

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