A 'light-up' intercalator displacement assay for detection of triplex DNA stabilizers

Chem Commun (Camb). 2020 Feb 13;56(13):1996-1999. doi: 10.1039/c9cc08817b.

Abstract

Here, we developed a coralyne-based, 'light-up' intercalator displacement assay to identify molecular stabilizers of triplex DNA using a sequence from a chromosomal breakpoint hotspot in the human c-MYC oncogene. Its potential to identify triplex DNA ligands was demonstrated using BePI and doxorubicin. Identification of triplex-interacting ligands may allow the regulation of genetic instability in human genomes.

MeSH terms

  • Berberine Alkaloids / chemistry
  • DNA / analysis*
  • DNA / chemistry
  • Doxorubicin / chemistry
  • Genome, Human
  • Genomic Instability
  • Humans
  • Indoles / chemistry
  • Intercalating Agents / chemistry*
  • Ligands
  • Proto-Oncogene Proteins c-myc / genetics
  • Pyridines / chemistry

Substances

  • Berberine Alkaloids
  • Indoles
  • Intercalating Agents
  • Ligands
  • Proto-Oncogene Proteins c-myc
  • Pyridines
  • triplex DNA
  • 3-methoxy-7H-8-methyl-11-((3'-amino)propylamino)benzo(e)pyrido(4,3-b)indole
  • coralyne
  • Doxorubicin
  • DNA