Information on the cellular internalization and stability of the ovarian cancer cell growth inhibitor peptide, LSCQLYQR (LR), is vital for lead optimization. Ad-hoc-synthesized LR/fluorescent-probe conjugates were used to monitor the internalization of the peptide. Mass spectrometry was used to identify adducts resulting from the thiol reactivity of the cysteine residue in LR. A mechanistic model is proposed to explain the observed change in intracellular peptide amount over time. Structural modifications can be foreseen to improve the peptide stability.
Internalization and stability of a thymidylate synthase peptide inhibitor in ovarian cancer cells / Cannazza, Giuseppe; Cazzato, ADDOLORATA STEFANIA; Marraccini, Chiara; Pavesi, Giorgia; Pirondi, Silvia; R., Guerrini; M., Pelà; Frassineti, Chiara; Ferrari, Stefania; Marverti, Gaetano; Ponterini, Glauco; Costi, Maria Paola. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 57:24(2014), pp. 10551-10556. [10.1021/jm501397h]
Internalization and stability of a thymidylate synthase peptide inhibitor in ovarian cancer cells
CANNAZZA, Giuseppe;CAZZATO, ADDOLORATA STEFANIA;MARRACCINI, CHIARA;PAVESI, Giorgia;PIRONDI, SILVIA;FRASSINETI, Chiara;FERRARI, Stefania;MARVERTI, Gaetano;PONTERINI, Glauco;COSTI, Maria Paola
2014
Abstract
Information on the cellular internalization and stability of the ovarian cancer cell growth inhibitor peptide, LSCQLYQR (LR), is vital for lead optimization. Ad-hoc-synthesized LR/fluorescent-probe conjugates were used to monitor the internalization of the peptide. Mass spectrometry was used to identify adducts resulting from the thiol reactivity of the cysteine residue in LR. A mechanistic model is proposed to explain the observed change in intracellular peptide amount over time. Structural modifications can be foreseen to improve the peptide stability.File | Dimensione | Formato | |
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LR internalization-J Med Chem 2014.pdf
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