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Bis-phenanthroline derivatives as suitable scaffolds for effective G-quadruplex recognition

2010; Royal Society of Chemistry; Volume: 39; Issue: 25 Linguagem: Inglês

10.1039/c0dt00038h

1477-9234

Sara Bianco, Caterina Musetti, Andrew R. Waldeck, Silvia Sparapani, Joshua D. Seitz, A. Paul Krapcho, Manlio Palumbo, Claudia Sissi,

RNA Interference and Gene Delivery

Selective recognition of DNA folding is central to multiple biological and pharmacological applications aimed at precise targeting of distinct genomic regions. Here, we focused on the recognition of physiologically relevant G-quadruplex (G-4) structures by bis-phenanthroline (bis-Phen) ligands containing two Phen moieties covalently linked through an amine or thioether bond. The transition metal ions Mn2+, Ni2+, Cu2+, and the biologically relevant Mg2+ and Zn2+ efficiently form 1 : 1 bis-Phen complexes characterised by a large planar structure fit to successfully recognise G-quartet arrangements.