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ChemMedChem. 2018 Sep 6;13(17):1755-1762. doi: 10.1002/cmdc.201800282. Epub 2018 Jul 18.

Toward Angiogenesis Inhibitors Based on the Conjugation of Organometallic Platinum(II) Complexes to RGD Peptides.

Author information

1
Departament de Química Inorgànica i Orgànica, Secció de Química Orgànica, IBUB, University of Barcelona, Martí i Franquès 1-11, 08028, Barcelona, Spain.
2
Departamento de Química Inorgánica, Universidad de Murcia and Institute for Bio-Health, Research of Murcia (IMIB-Arrixaca), 30071, Murcia, Spain.
3
Departament de Biologia, Universitat de Girona, 17071, Girona, Spain.
4
Biomed Division, LEITAT Technological Center, 08028, Barcelona, Spain.

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.

KEYWORDS:

angiogenesis; cancer; inhibitors; peptides; platinum

PMID:
29932312
DOI:
10.1002/cmdc.201800282

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