Abstract

Target-specific fluorescent probes that selectively bind to biologically important macromolecules, such as lipids, proteins, carbohydrates, and nucleic acids with special structures, can offer a powerful molecular tool for real-time study of their subcellular localization and dynamics of these biomolecules with advanced microscopy techniques1-4. DNA G4-structures from human c-MYC promoter is considered as important drug targets5-9; however, the developing of small-molecule-based fluorescent binding ligands that are highly selective targeting these G4-structures over other types of nucleic acids is challenging10-12. Herein, a small-sized c-MYC promoter G-quadruplex selective fluorescent BZT-Indolium binding ligand was demonstrated for the first time as a highly target-specific and photostable probe for in vitro staining and live cell imaging and it was found to be able to inhibit the amplification of the c-MYC G-rich sequence (G-quadruplex) and down-regulate oncogene c-MYC expression in HeLa cancer cells.

Reference：

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