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• W2015598957 abstract "The potential formation of G-quadruplexes in many regions of the genome makes them an attractive target for drug design. A large number of small molecules synthesized in recent years display an ability to selectively target and stabilize G-quadruplexes. To screen for G4 ligands, we modified a G4-FID (G-quadruplex Fluorescent Intercalator Displacement) assay. This test is based on the displacement of an “on/off” fluorescence probe, Thiazole Orange (TO), from quadruplex or duplex DNA matrices by increasing amounts of a putative ligand. Selectivity measurements can easily be achieved by comparing the ability of the ligand to displace TO from various quadruplex and duplex structures. G4-FID requires neither modified oligonucleotides nor specific equipment and is an isothermal experiment. This test was adapted for high throughput screening onto 96-well plates allowing the comparison of more than twenty different structures. Fifteen different known G4 ligands belonging to different families were tested. Most compounds showed a good G4 vs duplex selectivity but exhibited little, if any, specificity for one quadruplex sequence over the others. The quest for the “perfect” specific G4 ligand is not over yet!" @default.
• W2015598957 created "2016-06-24" @default.
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• W2015598957 date "2011-08-01" @default.
• W2015598957 modified "2023-10-14" @default.
• W2015598957 title "Fluorescence intercalator displacement assay for screening G4 ligands towards a variety of G-quadruplex structures" @default.
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• W2015598957 doi "https://doi.org/10.1016/j.biochi.2011.05.011" @default.
• W2015598957 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21641961" @default.
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