Publications by authors named "Addolorata Stefania Cazzato"
Article Synopsis
- The study focuses on designing lead drug conjugates combining folic acid and anticancer peptides to effectively target human thymidylate synthase (hTS) in cancer cells through the folate receptor α (FRα).
- These conjugates demonstrated a significantly higher binding affinity to the hTS monomer interface compared to the traditional enzyme active site, with proven effectiveness in cancer cell models at nanomolar concentrations.
- Unlike conventional drugs like 5-fluorouracil, which can cause the overexpression of hTS and lead to drug resistance, these conjugates do not trigger this response, making them a promising option in cancer treatment.
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.
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