Selective delivery of G-quadruplex ligand in glioma cell lines: the power of cyclic-RGD peptide.

ABSTRACT: Compounds targeting non-canonical secondary structures of nucleic acids, known as G-quadruplexes, are highly cytotoxic, both for cancer and healthy cells, because of their action mechanism's lack of appropriate selectivity. The targeted delivery of cytotoxic molecules to cancer cells is a valuable strategy to expand the repertoire of potential drugs, especially for cancer types for which new therapeutic tools are urgently needed, like glioblastoma. In this work, we conjugated a cyclic arginyl-glycyl-aspartic acid peptide to a naphthalene diimide, previously described as a highly performing stabilizing ligand for DNA G-quadruplexes, to specifically target glioma cells overexpressing RGD-binding integrin receptors. Our results, including confocal microscopy and cell toxicity assays, demonstr

SUBMITTER: Pirota V 

PROVIDER: S-EPMC11618373 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature