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Branched α-helical peptides enhanced antitumor efficacy and selectivity

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Abstract

Drug resistance to traditional chemotherapeutics is one of the main challenges in cancer treatment. Herein, cationic antimicrobial peptides (CAPs) were repurposed as anticancer agents to counter chemotherapy drug resistance. After a systematic study of de novo designed synthetic α-helical CAPs in various cell lines, the 4-arm branched peptide {[(LLKK)2]2κC}2 was found to exhibit better selectivity compared to its linear counterpart (LLKK)4, and was more effective than the 2-arm branched peptide [(LLKK)2]2κC. In particular, the 4-arm branched peptide could counter drug resistance and kill multiple drug resistant cells. Mechanism studies reveal that these α-helical peptides killed both the parent and resistant cancer cells based on the apoptotic pathway. The in vivo study in mice bearing breast tumors showed that branched peptides could be retained at the tumour sites after intratumoral injection and significantly reduced tumor growth while exhibiting minimal toxicity on main organs. These results indicate that the 4-arm branched peptide is a promising candidate for anticancer therapy.

Graphical abstract: Branched α-helical peptides enhanced antitumor efficacy and selectivity

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Article information


Submitted
20 Apr 2020
Accepted
31 Aug 2020
First published
08 Sep 2020

Biomater. Sci., 2020, Advance Article
Article type
Paper

Branched α-helical peptides enhanced antitumor efficacy and selectivity

X. Wang, Y. Zheng, C. Bao, G. Zhong, S. Liu, N. Wiradharma, W. Fan, Y. Y. Yang, X. Wang and Y. Huang, Biomater. Sci., 2020, Advance Article , DOI: 10.1039/D0BM00629G

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