방사선의학 웹진

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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.​ 

Author information

Lee D1, Lee SH2, Na Y2, Noh I1, Ha J1, Yoo J1, Bang HB1, Park JH1, Jeong KJ1, Yun CO3, Kim YC4.

1Department of Chemical and Biomolecular Engineering, Korea Advanced Institute of Science and Technology (KAIST), Daejeon, Republic of Korea.2Department of Bioengineering, College of Engineering, Hanyang University, Seoul, Republic of Korea.3Department of Bioengineering, College of Engineering, Hanyang University, Seoul, Republic of Korea. Electronic address: chaeok@hanyang.ac.kr.4Department of Chemical and Biomolecular Engineering, Korea Advanced Institute of Science and Technology (KAIST), Daejeon, Republic of Korea. Electronic address: dohnanyi@kaist.ac.kr.