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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, GANDIOSO, Albert, MASSAGUER I VALL-LLOVERA, Anna, BUENESTADO, Silvia, CALVIS, Carme, HERNÁNDEZ, José luis, MITJANS, Francesc, RODRÍGUEZ, Venancio, RUIZ, José, MARCHÁN SANCHO, Vicente. Toward angiogenesis inhibitors based on the conjugation of organometallic platinum(II) complexes to RGD peptides. _ChemMedChem_. 2018. Vol. 13, núm. 17, pàgs. 1755-1762. [consulta: 23 de gener de 2026]. ISSN: 1860-7179. [Disponible a: https://hdl.handle.net/2445/124909]

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