Development of a fluorescent intercalator displacement assay (G4-FID) for establishing quadruplex-DNA affinity and selectivity of putative ligands

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4842-5. doi: 10.1016/j.bmcl.2006.06.067. Epub 2006 Jul 11.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • DNA / analysis*
  • DNA / chemistry*
  • Fluorescent Dyes / chemical synthesis*
  • Fluorescent Dyes / chemistry
  • G-Quadruplexes
  • Ligands
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Fluorescent Dyes
  • Ligands
  • DNA