Ligands playing musical chairs with G-quadruplex DNA: A rapid and simple displacement assay for identifying selective G-quadruplex binders

  • D. Monchaud
  • , C. Allain
  • , H. Bertrand
  • , N. Smargiasso
  • , F. Rosu
  • , V. Gabelica
  • , A. De Cian
  • , J. L. Mergny
  • , M. P. Teulade-Fichou

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)1207-1223
Number of pages17
JournalBiochimie
Volume90
Issue number8
DOIs
Publication statusPublished - 1 Aug 2008
Externally publishedYes

Keywords

  • Fluorescent intercalator displacement
  • G-quadruplex DNA
  • G-quadruplex ligands
  • Thiazole orange

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