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

Borrelli, A.; Schiattarella, A.; Mancini, Roberto; Pica, A.; Pollio, M.L.; Ruggiero, M.G.; Bonelli, P.; De Luca, V.; Tuccillo, F.M.; Capasso, C.; Gori, E.; Sanseverino, M.; Carpentieri, A.; Birolo, L.; Pucci, P.; Rommelaere, J.; Mancinia, A.

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.

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Borrelli, A. / Schiattarella, A. / Mancini, Roberto / et al: A new hexapeptide from the leader peptide of rMnSOD enters cells through the oestrogen receptor to deliver therapeutic molecules. 2016.

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