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Interaction of an Acridine Dimer with DNA Quadruplex Structures

2001; Taylor & Francis; Volume: 19; Issue: 3 Linguagem: Inglês

10.1080/07391102.2001.10506758

1538-0254

Patrizia Alberti, Jinsong Ren, Marie‐Paule Teulade‐Fichou, Lionel Guittat, Jean‐François Riou, Jonathan B. Chaires, Claude Hélène, Jean‐Pierre Vigneron, Jean‐Maríe Lehn, Jean‐Louis Mergny,

RNA Interference and Gene Delivery

Abstract The reactivation of telomerase activity in most cancer cells supports the concept that telomerase is a relevant target in oncology, and telomerase inhibitors have been proposed as new potential anticancer agents. The telomeric G-rich single-stranded DNA can adopt an intramolecular G-quadruplex structure in vitro, which has been shown to inhibit telomerase activity. The C-rich sequence can also adopt a quadruplex (intercalated) structure (i-DNA). Two acridine derivatives were shown to increase the melting temperature of the G-quadruplex and the C-quadruplex at 1 μM dye concentration. The increase in Tm value of the G- quadruplex was associated with telomerase inhibition in vitro. The most active compound, “BisA”. showed an IC50 value of 0.75 μM in a standard TRAP assay.