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Non-conventional trans-platinum complexes functionalized with RDG peptides: chemical and cytototoxicity studies

Medrano, M. Angeles, Morais, Mauricio D.S., Ferreira, Vera, Correia, João D. G., Paulo, Antonio Rocha, Do Santos, Isabel, Navarro-Ranninger, Carmen, Alvarez-Valdes, Amparo, Casini, Angela, Mendes, Filipa and Gomez Quiroga, Adoracion 2017. Non-conventional trans-platinum complexes functionalized with RDG peptides: chemical and cytototoxicity studies. European Journal of Inorganic Chemistry 12 , pp. 1835-1840. 10.1002/ejic.201700072

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In order to target platinum complexes to cancer cells, trans-Pt(II) or trans-Pt(IV) complexes were bioconjugated to the cyclic peptide cRGDfK (cRGD), with affinity for αvβ3 integrin receptors, through their 4-picolinic acid spectator ligands. To tackle this goal, the Pt(II) and Pt(IV) precursors were activated at their carboxylic acid function and futher reacted with the cRGDfK peptide, to afford the bioconjugates Pt(II)-cRGD and Pt(IV)-cRGD, respectively. Pt(II)-cRGD was studied by 195Pt-NMR that confirmed the presence of the Pt(II) center. In contrast, the characterization of Pt(IV)-cRGD was not possible due to the tendency of this complex to undergo reduction to Pt(II) in solution. Thus, only the Pt(II)-cRGD complex was used for further biological studies, and it exhibited some cytotoxic activity against the HUVEC cell line, with the highest levels of αvβ3 expression. However, no improved effects were observed with respect to the Pt(II)-pic precursor. Studies by ICP-MS showed enhanced intracellular accumulation for Pt(II)-cRGD with respect to Pt(II)-pic in cancer cells. Overall, these results show that while Pt(II) bioconjugation enhances compound's uptake, it did not translate into an increase in cytotoxicity.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
Uncontrolled Keywords: platinum complexes, anticancer drugs, peptides, cytotoxicity
Publisher: Wiley
ISSN: 1434-1948
Date of First Compliant Deposit: 14 February 2017
Date of Acceptance: 6 February 2017
Last Modified: 28 Nov 2020 10:34

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