title: Ligands playing musical chairs with G-quadruplex DNA: a rapid and simple displacement assay for identifying selective G-quadruplex binders.
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.
authors.affiliation: Institut Curie, Section Recherche, CNRS UMR176, Centre Universitaire Paris XI, Bat. 110, 91405 Orsay, France.
authors.forename: D
authors.initials: D
authors.lastname: Monchaud
authors.forename: C
authors.initials: C
authors.lastname: Allain
authors.forename: H
authors.initials: H
authors.lastname: Bertrand
authors.forename: N
authors.initials: N
authors.lastname: Smargiasso
authors.forename: F
authors.initials: F
authors.lastname: Rosu
authors.forename: V
authors.initials: V
authors.lastname: Gabelica
authors.forename: A
authors.initials: A
authors.lastname: De Cian
authors.forename: J-L
authors.initials: JL
authors.lastname: Mergny
authors.forename: M-P
authors.initials: MP
authors.lastname: Teulade-Fichou
mesh_terms: D000166:Acridines / Q000737:chemistry / Q000378:metabolism; D001483:Base Sequence; D052160:Benzothiazoles / Q000378:metabolism; D004247:DNA / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism*; D054856:G-Quadruplexes; D008024:Ligands; D009841:Oligonucleotides / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D009942:Organometallic Compounds / Q000378:metabolism; D011804:Quinolines / Q000378:metabolism; D011806:Quinolinium Compounds / Q000378:metabolism; D012492:Salts / Q000494:pharmacology; D012680:Sensitivity and Specificity; D013997:Time Factors
chemical_list: D000166:Acridines; D052160:Benzothiazoles; D008024:Ligands; D009841:Oligonucleotides; D009942:Organometallic Compounds; D011804:Quinolines; D011806:Quinolinium Compounds; D012492:Salts; C051000:thiazole orange; D004247:DNA