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.
A new hexapeptide from the leader peptide of rMnSOD enters cells through the oestrogen receptor to deliver therapeutic molecules / Borrelli, A.; Schiattarella, A.; Mancini, R.; Pica, Alessandra; Pollio, MARIA LAURA; Ruggiero, MARIA GRAZIA; Bonelli, P.; De Luca, V.; Tuccillo, F. M.; Capasso, Clemente; Gori, E.; Sanseverino, M.; Carpentieri, Andrea; Birolo, Leila; Pucci, Pietro; Rommelaere, J.; Mancini, A.. - In: SCIENTIFIC REPORTS. - ISSN 2045-2322. - 6:(2016), pp. 18691-18703. [10.1038/srep18691]
A new hexapeptide from the leader peptide of rMnSOD enters cells through the oestrogen receptor to deliver therapeutic molecules
PICA, ALESSANDRA;POLLIO, MARIA LAURA;RUGGIERO, MARIA GRAZIA;CAPASSO, CLEMENTE;CARPENTIERI, ANDREA;BIROLO, LEILA;PUCCI, PIETRO;
2016
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.File | Dimensione | Formato | |
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