Development of a fluorescent ligand that can illuminate nuclear G-quadruplexes and modulate oncogene expression.
Bioorg Med Chem
; 104: 117713, 2024 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-38574409
ABSTRACT
In this study, we developed a promising dual-function fluorescent ligand termed KS-1 by a slight structural modification on a reported carbazole-based scaffold. KS-1 was then found to mainly bind and illuminate the nuclear DNA G-quadruplexes (G4s) in a sandwich-like interacting mode, and also effectively modulate the oncogene expression through a G4-mediated manner. Furthermore, KS-1 was proved to inhibit cancer cell growth either in 2D monolayer cells or 3D multicellular tumor spheroids. To be noted, this ligand could overcome the shortcomings of other reported dual-function ligands that appeared to accumulate in the lysosomes or mitochondria, and may be used as a theranostic agent in the future.
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Base de dados:
MEDLINE
Assunto principal:
Quadruplex G
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article