A new hexapeptide from the leader peptide of rMnSOD enters cells through the oestrogen receptor to deliver therapeutic molecules

Antonella Borrelli, Antonietta Schiattarella, Roberto Mancini, Alessandra Pica, Maria Laura Pollio, Patrizia Bonelli, Franca Maria Tuccillo, Clemente Capasso, Enrico Gori, Marina Sanseverino, Andrea Carpentieri, Leila Birolo, Piero Pucci, Jean Rommelaere, Aldo Mancini

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Abstract

A 24-amino acid leader peptide of a new human recombinant manganese superoxide dismutase can enter cells and carry molecules. Here, we demonstrated that six of the 24 amino acids penetrate cells through a particular gate represented by a specific amino acid sequence of the oestrogen receptor (ER). We analysed the internalization of the synthetic hexapeptide and the cytotoxic activity of the hexapeptide conjugated to cisplatin on a cell line panel. In most cell lines, the hexapeptide delivered an amount of cisplatin that was 2 to 8 times greater than that released by cisplatin when the drug was used alone. This increased delivery increases the therapeutic index of cisplatin and reduces side effects caused by a high dosage or long-term treatment times. We may consider this hexapeptide a new molecular carrier to deliver molecules with therapeutic activity into ER + cells for diagnostic purposes and clinical or immune therapy.

Original languageEnglish
Article number18691
JournalScientific Reports
Volume6
DOIs
Publication statusPublished - Jan 4 2016

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Cite this

Borrelli, A., Schiattarella, A., Mancini, R., Pica, A., Pollio, M. L., Bonelli, P., Tuccillo, F. M., Capasso, C., Gori, E., Sanseverino, M., Carpentieri, A., Birolo, L., Pucci, P., Rommelaere, J., & Mancini, A. (2016). A new hexapeptide from the leader peptide of rMnSOD enters cells through the oestrogen receptor to deliver therapeutic molecules. Scientific Reports, 6, [18691]. https://doi.org/10.1038/srep18691