Internalization and stability of a thymidylate synthase peptide inhibitor in ovarian cancer cells
Articolo
Data di Pubblicazione:
2014
Citazione:
Internalization and stability of a thymidylate synthase peptide inhibitor in ovarian cancer cells / Cannazza, G., Cazzato, A.S., Marraccini, C., Pavesi, G., Pirondi, S., R., G., M., P., Frassineti, C., Ferrari, S., Marverti, G., Ponterini, G., Costi, M.P.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 57:24(2014), pp. 10551-10556. [10.1021/jm501397h]
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.
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.
Tipologia CRIS:
Articolo su rivista
Keywords:
Cell Proliferation; Enzyme Inhibitors; Female; Fluorescence; Humans; Microscopy, Confocal; Molecular Structure; Ovarian Neoplasms; Peptide Fragments; Tandem Mass Spectrometry; Thymidylate Synthase; Tumor Cells, Cultured; Molecular Medicine; Drug Discovery3003 Pharmaceutical Science; Medicine (all)
Elenco autori:
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
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