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Title: Toward Angiogenesis Inhibitors Based on the Conjugation of Organometallic Platinum(II) Complexes to RGD Peptides. Author: Zamora A, Gandioso A, Massaguer A, Buenestado S, Calvis C, Hernández JL, Mitjans F, Rodríguez V, Ruiz J, Marchán V. Journal: ChemMedChem; 2018 Sep 06; 13(17):1755-1762. PubMed ID: 29932312. Abstract: 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.[Abstract] [Full Text] [Related] [New Search]