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Toward angiogenesis inhibitors based on the conjugation of organometallic platinum(II) complexes to RGD peptides
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A novel conjugate between a cyclometalated platinum(II) complex with dual antiangiogenic and antitumor activity and a cyclic peptide containing the RGD sequence (-Arg-Gly-Asp-) has been synthesized by combining solid- and solution-phase methodologies. Although peptide conjugation rendered a non-cytotoxic compound in all tested tumor cell lines (± αV β3 and αV β5 integrin receptors), the antiangiogenic activity of the Pt-c(RGDfK) conjugate in human umbilical vein endothelial cells at sub-cytotoxic concentrations opens the way to the design of a novel class of angiogenesis inhibitors through conjugation of metallodrugs with high antiangiogenic activity to cyclic RGD-containing peptides or peptidomimetic analogues.
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ZAMORA, Ana, et al. Toward angiogenesis inhibitors based on the conjugation of organometallic platinum(II) complexes to RGD peptides. ChemMedChem. 2018. Vol. 13, num. 17, pags. 1755-1762. ISSN 1860-7179. [consulted: 19 of August of 2026]. Available at: https://hdl.handle.net/2445/124909