Increasing the potential of cell-penetrating peptides for cancer therapy using a new pentagonal scaffold

• Type: Article in International Scientific Journal
• Date: 2019

Authors

Duarte, D (Author) Other; Fraga, AG (Author) Other; Pedrosa, J (Author) Other; Martel, F (Author) FMUP; Nuno Vale (Author) ICBAS

Journal

Title: European Journal of Pharmacology

Vol. 860

ISSN: 0014-2999

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 3 Citations

Scopus - 5 Citations

Other information

Authenticus ID: P-00Q-WB7

DOI: 10.1016/j.ejphar.2019.172554

Abstract (EN): Cancer treatment is one of the major fields of interest for the scientific community. Investment in cancer research is costly but essential to provide patients with more effective and safe treatments. In this project, we describe the synthesis and characterization of new thiazole derivatives coupled to CPP2, a cell-penetrating peptide (CPP) reported for colon cancer cells. Using a human adenocarcinoma-derived cell line (Caco-2), these new CPPs were evaluated for antiproliferative (H-3-thymidine incorporation) and cytotoxic effect (extracellular lactate dehydrogenase activity). One of these derivatives, the BTZCA thiazole compound and its peptide-conjugated (BTZCA-CPP2) also showed the ability to decrease tumour cell viability and proliferation, with potential cytotoxic effect against human breast cancer MCF-7 cells. Then, cytotoxicity studies were developed against J774, L929 and THP1 cell lines and this new family showed no significant cytotoxicity, when compared to their counterparts alone (BTZCA and CPP2). The use of smaller CPP conjugated with this family of derivatives can be also considered in future for the development of new drugs to cancer therapy.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 11