期刊
CHEMMEDCHEM
卷 13, 期 17, 页码 1755-1762出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201800282
关键词
angiogenesis; cancer; inhibitors; peptides; platinum
资金
- Spanish Ministry of Economy and Competitiveness
- FEDER funds [CTQ2014-52658-R, CTQ2015-64319-R, CTQ2017-84779-R]
- COST [CM1105]
- Fundacion Seneca-CARM [19020/FPI/13]
- University of Barcelona
- University of Girona [MPCUdG2016/076]
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 (+/- (V3) and (V5) 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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