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Issue 42, 2016
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Clioquinol–ruthenium complex impairs tumour cell invasion by inhibiting cathepsin B activity

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Abstract

Over the past few years, the organometalled compounds, including ruthenium, gained a lot of attention as anticancer agents. We report on the clioquinol–ruthenium complex [Ru(η6-p-cymene)(Cq)Cl] as a potent inhibitor of cathepsin B, a lysosomal cysteine peptidase, involved in tumour cell invasion and metastasis. In the low micromolar concentration range, the clioquinol–ruthenium complex did not exhibit cytotoxic effects on MCF-10A neoT and U-87 MG cells; it did, however, significantly reduce their ability for extracellular matrix degradation and invasiveness in two independent cell-based models, measuring either electrical impedance in real time or the growth of multicellular tumour spheroids implanted in Matrigel, a model representing the extracellular matrix. These results establish ruthenium based organometallic compounds as promising candidates for further pre-clinical studies as anticancer therapeutics.

Graphical abstract: Clioquinol–ruthenium complex impairs tumour cell invasion by inhibiting cathepsin B activity

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Publication details

The article was received on 14 Jun 2016, accepted on 16 Sep 2016 and first published on 16 Sep 2016


Article type: Paper
DOI: 10.1039/C6DT02369J
Citation: Dalton Trans., 2016,45, 16913-16921
  • Open access: Creative Commons BY-NC license
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    Clioquinol–ruthenium complex impairs tumour cell invasion by inhibiting cathepsin B activity

    A. Mitrović, J. Kljun, I. Sosič, S. Gobec, I. Turel and J. Kos, Dalton Trans., 2016, 45, 16913
    DOI: 10.1039/C6DT02369J

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