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A novel biosensing strategy for screening G-quadruplex ligands based on graphene oxide sheets
Haibo Wang1, Tingting Chen, Shuang Wu
1State Key Laboratory for Chemo/biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, PR China.
Biosensors & Bioelectronics
|February 17, 2012
Summary
A new fluorescence biosensing method uses graphene oxide to quickly and sensitively select potential G-quadruplex-binding ligands. This approach aids in discovering new anticancer drugs from natural compounds.
Area of Science:
- Biochemistry
- Materials Science
- Drug Discovery
Background:
- G-quadruplex structures are crucial in biological processes and disease.
- Identifying ligands that bind to G-quadruplexes is vital for developing new therapeutics, particularly anticancer drugs.
- Existing methods for screening G-quadruplex ligands can be complex and time-consuming.
Purpose of the Study:
- To develop a simple, rapid, and sensitive fluorescence biosensing strategy for selecting quadruplex-binding ligands.
- To utilize graphene oxide (GO) as an effective fluorescence quencher in this biosensing system.
- To validate the method by screening Chinese medicine monomers for G-quadruplex binding activity.
Main Methods:
- Preparation and characterization of single-layered graphene oxide (GO) sheets using TEM, AFM, FT-IR, and Raman spectroscopy.
- Design of a fluorescein amidite (FAM)-labeled signal probe that adsorbs to GO via π-stacking, leading to fluorescence quenching.
- Detection of quadruplex-binding ligands based on the recovery of FAM fluorescence upon probe release from GO due to G-quadruplex formation.
Main Results:
- Successfully synthesized and characterized well-dispersed single-layered GO sheets.
- Demonstrated that the FAM-labeled probe's fluorescence is quenched by GO and recovered upon ligand introduction.
- Identified flavonoids from Chinese medicine monomers as potential G-quadruplex-binding ligands through fluorescence measurements and melting temperature analysis.
Conclusions:
- The proposed fluorescence biosensing strategy is simple, rapid, and sensitive for screening G-quadruplex ligands.
- This method shows significant potential for the discovery of novel anticancer drugs targeting G-quadruplex structures.
- The findings highlight the utility of graphene oxide in developing advanced biosensing platforms for drug discovery.
