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

GUERRINI, Remo;
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.
2014
Cannazza, G; Cazzato, As; Marraccini, C; Pavesi, G; Pirondi, S; Guerrini, Remo; Pela, M; Frassineti, C; Ferrari, S; Marverti, G; Ponterini, G; Costi, Mp
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/2338793
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