6533b830fe1ef96bd129685a
RESEARCH PRODUCT
Another step toward DNA selective targeting: NiII and CuII complexes of a Schiff base ligand able to bind gene promoter G-quadruplexes
Walter BergerGiampaolo BaroneAlessio TerenziAlessio TerenziSushilla Van SchoonhovenDaniela LötschBernhard K. KepplerBernhard K. KepplerAlexander RollerChristian R. KowolChristian R. Kowolsubject
Circular dichroismSchiff base010405 organic chemistryStereochemistryChemistryLigandPromoter010402 general chemistryG-quadruplex01 natural sciences3. Good health0104 chemical sciencesInorganic Chemistrychemistry.chemical_compoundFörster resonance energy transferLipofectamineSettore CHIM/03 - Chimica Generale E InorganicaDNAdescription
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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2016-05-14 |