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Functionalization of Ruthenium(II) terpyridine complexes with cyclic RGD peptides to target integrin receptors in cancer cells

Hahn, Eva, Estrada-Ortiz, Natalia, Han, Jiaying, Ferreira, Vera F. C., Kapp, Tobias, Correia, Joao D. G., Casini, Angela and Kühn, Fritz E. 2017. Functionalization of Ruthenium(II) terpyridine complexes with cyclic RGD peptides to target integrin receptors in cancer cells. European Journal of Inorganic Chemistry 2017 (12) , pp. 1667-1672. 10.1002/ejic.201601094

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The lack of selectivity for cancer cells and the resulting negative impact on healthy tissue is a severe drawback of actual cancer chemotherapy. Tethering of cytotoxic drugs to targeting vectors such as peptides, which recognize receptors overexpressed on the surface of tumor cells, is one possible strategy to overcome such a problem. The pentapeptide cyc(RGDfK) targets the integrin receptor αvβ3, important for tumor growth and metastasis formation. In this work, two terpyridine based Ru(II) complexes were prepared and for the first time conjugated to cyc(RGDfK) via amide bond formation resulting in a monomeric and a dimeric bioconjugate. Both Ru(II) complexes bind strongly and selectively to integrin αvβ3, with the dimeric molecule displaying a 20-fold higher affinity to the receptor than the monomeric one. However, the cytotoxicity of the complexes and related bioconjugates against human A549 and SKOV-3 cell lines is still not sufficient for application as anticancer agents. Nevertheless, considering the high selectivity for integrin receptor αvβ3, the synthesis of Ru-based bioconjugates with cyc(RGDfK) paves a promising way towards the design of effective targeted anticancer agents.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
Uncontrolled Keywords: tumor targeting peptide • ruthenium • antitumor agent • bioconjugation • RGD
Publisher: Wiley
ISSN: 1434-1948
Date of First Compliant Deposit: 14 November 2016
Date of Acceptance: 8 November 2016
Last Modified: 19 Jan 2021 18:48

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