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Title: Toward angiogenesis inhibitors based on the conjugation of organometallic platinum(II) complexes to RGD peptides
Author: 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
Keywords: Angiogènesi
Compostos organometàl·lics
Organometallic compounds
Issue Date: 6-Sep-2018
Publisher: Wiley-VCH
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.
Note: Versió postprint del document publicat a:
It is part of: ChemMedChem, 2018, vol. 13, num. 17, p. 1755-1762
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ISSN: 1860-7179
Appears in Collections:Articles publicats en revistes (Química Inorgànica i Orgànica)

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