期刊
BIOCHIMIE
卷 93, 期 8, 页码 1288-1296出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.biochi.2011.05.011
关键词
Quadruplex; DNA-DNA ligand interactions; Fluorescence; Screening assay
资金
- ANR [G4-TOOLBOX, ANR-Blan-09-355]
- Universite Bordeaux Segalen - MESR
- Institut Curie
- Centre National de la Recherche Scientifique
- Region Aquitaine
- Fondation pour la Recherche Medicale (FRM)
- Association Francaise de l'Ataxie de Friedreich (AFAF)
- INCa
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! (C) 2011 Elsevier Masson SAS. All rights reserved.
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