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Effect of trimethine cyanine dye- and folate-conjugation on the in vitro biological activity of proapoptotic peptides

Cardella, Davide, Deng, Wenjing, Luk, Louis Y. P. and Tsai, Yu-Hsuan 2022. Effect of trimethine cyanine dye- and folate-conjugation on the in vitro biological activity of proapoptotic peptides. Biomolecules 12 (5) , 725. 10.3390/biom12050725

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Abstract

Despite continuous advances, anticancer therapy still faces several technical hurdles, such as selectivity on cellular and subcellular targets of therapeutics. Toward addressing these limitations, we have combined the use of proapoptotic peptides, trimethine cyanine dye, and folate to target the mitochondria of tumor cells. A series of proapoptotic peptides and their conjugates with a cyanine dye and/or folate were synthesized in the solid phase, and their toxicity in different human cell lines was assessed. Cyanine-bearing conjugates were found to be up to 100-fold more cytotoxic than the parent peptides and to localize in mitochondria. However, the addition of a folate motif did not enhance the potency or selectivity of the resulting conjugates toward tumor cells that overexpress folate receptor α. Furthermore, while dual-labeled constructs were also found to localize within the target organelle, they were not generally selective towards folate receptor α-positive cell lines in vitro.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Chemistry
Additional Information: License information from Publisher: LICENSE 1: URL: https://creativecommons.org/licenses/by/4.0/
Publisher: MDPI
Date of First Compliant Deposit: 24 May 2022
Date of Acceptance: 16 May 2022
Last Modified: 30 Jun 2022 08:41
URI: https://orca.cardiff.ac.uk/id/eprint/150010

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