Conformation-switchable helical polypeptide eliciting selective pro-apoptotic activity for cancer therapy
- Authors
- Lee, DaeYong; Lee, Soo-Hwan; Na, Youjin; Noh, Ilkoo; Ha, JongHoon; Yoo, Jisang; Bang, Hyun Bae; Park, Jong Hyun; Jeong, Ki Jun; Yun, Chae-Ok; Kim, Yeu-Chun
- Issue Date
- Oct-2017
- Publisher
- ELSEVIER SCIENCE BV
- Keywords
- pH-activated helical formation; Mitochondrial membrane destabilization; Pro-apoptotic activity; Cancer targeting and therapy
- Citation
- JOURNAL OF CONTROLLED RELEASE, v.264, pp.24 - 33
- Indexed
- SCIE
SCOPUS
- Journal Title
- JOURNAL OF CONTROLLED RELEASE
- Volume
- 264
- Start Page
- 24
- End Page
- 33
- URI
- https://scholarworks.bwise.kr/hanyang/handle/2021.sw.hanyang/5378
- DOI
- 10.1016/j.jconrel.2017.08.001
- ISSN
- 0168-3659
- 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.
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