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Issue 18, 2016
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Another step toward DNA selective targeting: NiII and CuII complexes of a Schiff base ligand able to bind gene promoter G-quadruplexes

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Abstract

DNA G-rich sequences are able to form four-stranded structures organized in stacked guanine tetrads. These structures, called G-quadruplexes, were found to have an important role in the regulation of oncogenes expression and became, for such a reason, appealing targets for anticancer drugs. Aiming at finding selective G-quadruplex binders, we have designed, synthesized and characterized a new water soluble Salen-like Schiff base ligand and its NiII and CuII metal complexes. UV-Vis, circular dichroism and FRET measurements indicated that the nickel complex can stabilize oncogene promoter G-quadruplexes with high selectivity, presenting no interactions with duplex DNA at all. The same compound exhibited dose-dependent cytotoxic activity in MCF-7 breast cancer cells when combined with lipofectamine as lipophilic carrier.

Graphical abstract: Another step toward DNA selective targeting: NiII and CuII complexes of a Schiff base ligand able to bind gene promoter G-quadruplexes

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Publication details

The article was received on 17 Feb 2016, accepted on 01 Apr 2016 and first published on 04 Apr 2016


Article type: Paper
DOI: 10.1039/C6DT00648E
Citation: Dalton Trans., 2016,45, 7758-7767
  • Open access: Creative Commons BY license
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    Another step toward DNA selective targeting: NiII and CuII complexes of a Schiff base ligand able to bind gene promoter G-quadruplexes

    A. Terenzi, D. Lötsch, S. van Schoonhoven, A. Roller, C. R. Kowol, W. Berger, B. K. Keppler and G. Barone, Dalton Trans., 2016, 45, 7758
    DOI: 10.1039/C6DT00648E

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