Small Molecule Fluorescent Probes for G- Quadruplex Visualization as Potential Cancer Theranostic Agents

Molecules. 2019 Feb 19;24(4):752. doi: 10.3390/molecules24040752.

Abstract

G-quadruplexes have gained prominence over the past two decades for their role in gene regulation, control of anti-tumour activity and ageing. The physiological relevance and significance of these non-canonical structures in the context of cancer has been reviewed several times. Putative roles of G-quadruplexes in cancer prognosis and pathogenesis have spurred the search for small molecule ligands that are capable of binding and modulating the effect of such structures. On a related theme, small molecule fluorescent probes have emerged that are capable of selective recognition of G-quadruplex structures. These have opened up the possibility of direct visualization and tracking of such structures. In this review we outline recent developments on G-quadruplex specific small molecule fluorescent probes for visualizing G-quadruplexes. The molecules represent a variety of structural scaffolds, mechanism of quadruplex-recognition and fluorescence signal transduction. Quadruplex selectivity and in vivo imaging potential of these molecules places them uniquely as quadruplex-theranostic agents in the predominantly cancer therapeutic context of quadruplex-selective ligands.

Keywords: G-quadruplex probe; G-quadruplexes; cancer theranostic; oncogene promoter; quadruplex visualization.

Publication types

  • Review

MeSH terms

  • Animals
  • Fluorescent Dyes* / chemistry
  • G-Quadruplexes*
  • Humans
  • Microscopy, Fluorescence
  • Molecular Imaging* / methods
  • Molecular Structure
  • Theranostic Nanomedicine* / methods

Substances

  • Fluorescent Dyes