A light-up probe targeting for Bcl-2 2345 G-quadruplex DNA with carbazole TO

Spectrochim Acta A Mol Biomol Spectrosc. 2018 Feb 15:191:180-188. doi: 10.1016/j.saa.2017.10.012. Epub 2017 Oct 4.

Abstract

As its significant role, the selective recognition of G-quadruplex with specific structures and functions is important in biological and medicinal chemistry. Carbazole derivatives have been reported as a kind of fluorescent probe with many excellent optical properties. In the present study, the fluorescence of the dye (carbazole TO) increased almost 70 fold in the presence of bcl-2 2345 G4 compared to that alone in aqueous buffer condition with almost no fluorescence and 10-30 fold than those in the presence of other DNAs. The binding study results by activity inhibition of G4/Hemin peroxidase experiment, NMR titration and molecular docking simulation showed the high affinity and selectivity to bcl-2 2345 G4 arises from its end-stacking interaction with G-quartet. It is said that a facile approach with excellent sensitive, good selectivity and quick response for bcl-2 2345 G-quadruplex was developed and may be used for antitumor recognition or antitumor agents.

Keywords: Bcl-2 2345 G-quadruplex; Carbazole TO; Fluorescent probe; Light up; Targeting.

MeSH terms

  • Base Sequence
  • Carbazoles / chemistry*
  • Circular Dichroism
  • DNA / chemistry*
  • Fluorescent Dyes / chemistry*
  • G-Quadruplexes*
  • Humans
  • Molecular Conformation
  • Molecular Docking Simulation
  • Proto-Oncogene Proteins c-bcl-2 / metabolism*
  • Proton Magnetic Resonance Spectroscopy
  • Quantum Theory
  • Spectrometry, Fluorescence
  • Time Factors

Substances

  • Carbazoles
  • Fluorescent Dyes
  • Proto-Oncogene Proteins c-bcl-2
  • carbazole
  • DNA