Development of a fluorescent intercalator displacement assay (G4-FID) for establishing quadruplex-DNA affinity and selectivity of putative ligands.
A fluorescent intercalator displacement assay (G4-FID) has been designed based on the displacement of thiazole orange (TO) positioned onto a quadruplex-forming oligonucleotide by putative ligands. This technique was validated by the use of a set of representative and fully characterized G-quadruplex binders (ranging from pyridodicarboxamide to macrocyclic ligands). To further extend its applicability, a comparative version has been developed which allows a rapid and viable determination of quadruplex- over duplex-selectivity.
Monchaud
David
D
Laboratoire de Chimie des Interactions Moléculaires, Collège de France, CNRS UPR285, 75005 Paris, France.
Allain
Clémence
C
Teulade-Fichou
Marie-Paule
MP
D004247:DNA / Q000032:analysis* / Q000737:chemistry*; D005456:Fluorescent Dyes / Q000138:chemical synthesis* / Q000737:chemistry; D054856:G-Quadruplexes; D008024:Ligands; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D005456:Fluorescent Dyes; D008024:Ligands; D004247:DNA