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Title: Ligands playing musical chairs with G-quadruplex DNA: a rapid and simple displacement assay for identifying selective G-quadruplex binders. Author: Monchaud D, Allain C, Bertrand H, Smargiasso N, Rosu F, Gabelica V, De Cian A, Mergny JL, Teulade-Fichou MP. Journal: Biochimie; 2008 Aug; 90(8):1207-23. PubMed ID: 18343231. Abstract: We report here the details of G4-FID (G-quadruplex fluorescent intercalator displacement), a simple method aiming at evaluating quadruplex-DNA binding affinity and quadruplex- over duplex-DNA selectivity of putative ligands. This assay is based on the loss of fluorescence upon displacement of thiazole orange from quadruplex- and duplex-DNA matrices. The original protocol was tested using various quadruplex- and duplex-DNA targets, and with a wide panel of G-quadruplex ligands belonging to different families (i.e. from quinacridines to metallo-organic ligands) likely to display various binding modes. The reliability of the assay is further supported by comparisons with FRET-melting and ESI-MS assays.[Abstract] [Full Text] [Related] [New Search]