title: Identification of trinucleotide repeat ligands with a FRET melting assay.
abstract: DNA hairpin structures formed within a repeated tract might be a causative factor for triplet expansion observed in several debilitating diseases. We have designed and used a fluorescence resonance energy transfer (FRET) melting assay to screen for ligands that bind specifically to the CNG triplet repeats. Using this assay, we screened a panel of 33 chemicals that were previously designed to bind DNA or RNA secondary structures. Remarkably, we found that macrocyclic compounds, such as acridine dimers and trimers, exhibit interesting affinities and specificities for this motif.
authors.affiliation: Muséum National d'Histoire Naturelle (MNHN) USM 503, INSERM U565, CNRS UMR 5153, Case Postale 26, 57 rue Cuvier 75005 Paris, France.
authors.forename: Samir
authors.initials: S
authors.lastname: Amrane
authors.forename: Anne
authors.initials: A
authors.lastname: De Cian
authors.forename: Frédéric
authors.initials: F
authors.lastname: Rosu
authors.forename: Markus
authors.initials: M
authors.lastname: Kaiser
authors.forename: Edwin
authors.initials: E
authors.lastname: De Pauw
authors.forename: Marie-Paule
authors.initials: MP
authors.lastname: Teulade-Fichou
authors.forename: Jean-Louis
authors.initials: JL
authors.lastname: Mergny
mesh_terms: D031541:Fluorescence Resonance Energy Transfer / Q000379:methods*; D008024:Ligands; D044366:Transition Temperature; D018911:Trinucleotide Repeats
chemical_list: D008024:Ligands