A Fluorescent Aptamer Sensor Based on Cu-TCPP/rGO for Homogeneous Screening of G-Quadruplex Ligands
- 1Xi’an International University , , , ,
- 2Northwest University , , , ,
Abstract
Single-stranded human telomeric DNA can fold into G-quadruplexes, structures composed of stacked G-quartets. Ligands that target G-quadruplex DNA have received considerable attention because of their potential anticancer activity. We developed a Förster resonance energy transfer (FRET) system to identify drugs that stabilize G-quadruplexes with human telomeric DNA in a homogeneous medium using Cu-4,4,4,4-(Porphine-5,10,15,20-tetrayl) tetrakis (benzoic acid)/reduced graphene oxide (Cu-TCPP/rGO) as fluorescence quencher. Fluorescein-tagged human telomeric G-rich DNA (F-GDNA) exhibited significant fluorescence quenching upon adsorption onto the Cu-TCPP/rGO surface, with fluorescence recovery observed when the ligands were bound to the G-quadruplexes. The ligand stabilized formation of G-quadruplexes was further confirmed using circular dichroism (CD) spectroscopy. Notably, flavonoids and anthraquinones derived from traditional Chinese medicines promoted G-quadruplex formation within the GDNA. The combined results of fluorescence and CD spectroscopy indicate that the proposed FRET-based methodology serves as a cost-effective, facile, and efficient tool for screening G-quadruplex ligands. This approach has significant potential for application in the identification of telomerase-targeting anticancer drugs.
Related
- Structural Empowerment Sensing: Decoding the Structure-Activity Relationship and Detection Application of G‑Quadruplex Aptamer.
- A Role for Janus Cyclohexyl Ring Motifs in Medicinal Chemistry. Incorporation Into G-Quadruplex Ligands and Anti-Trypanosoma brucei Activity.
- Repurposing dopamine D3 receptor fluorescent ligands for D2 receptor
- Organic compounds as Photosystem II inhibitors and Cu²⁺ ligands: insights from primary screening.
- Chapter 14: Unwinding Quadruplex Structures with RNA Helicases
BibTeX
@article{chen2026fluorescent,
title = {{A Fluorescent Aptamer Sensor Based on Cu-TCPP/rGO for Homogeneous Screening of G-Quadruplex Ligands}},
author = {Guozhen Chen and Jiaxin Li and Jianbin Zheng},
journal = {ACS Omega},
year = {2026},
month = oct,
doi = {10.1021/acsomega.6c02294},
url = {https://pubs.acs.org/acsodf/article/11/41/62533/5448473/A-Fluorescent-Aptamer-Sensor-Based-on-Cu-TCPP-rGO},
note = {CC BY-NC-ND 4.0},
}
RIS
TY - JOUR
TI - A Fluorescent Aptamer Sensor Based on Cu-TCPP/rGO for Homogeneous Screening of G-Quadruplex Ligands
AU - Guozhen Chen
AU - Jiaxin Li
AU - Jianbin Zheng
PY - 2026
DA - 2026/10/10
JO - ACS Omega
DO - 10.1021/acsomega.6c02294
UR - https://pubs.acs.org/acsodf/article/11/41/62533/5448473/A-Fluorescent-Aptamer-Sensor-Based-on-Cu-TCPP-rGO
AB - Single-stranded human telomeric DNA can fold into G-quadruplexes, structures composed of stacked G-quartets. Ligands that target G-quadruplex DNA have received considerable attention because of their potential anticancer activity. We developed a Förster resonance energy transfer (FRET) system to identify drugs that stabilize G-quadruplexes with human telomeric DNA in a homogeneous medium using Cu-4,4,4,4-(Porphine-5,10,15,20-tetrayl) tetrakis (benzoic acid)/reduced graphene oxide (Cu-TCPP/rGO) as fluorescence quencher. Fluorescein-tagged human telomeric G-rich DNA (F-GDNA) exhibited significant fluorescence quenching upon adsorption onto the Cu-TCPP/rGO surface, with fluorescence recovery observed when the ligands were bound to the G-quadruplexes. The ligand stabilized formation of G-quadruplexes was further confirmed using circular dichroism (CD) spectroscopy. Notably, flavonoids and anthraquinones derived from traditional Chinese medicines promoted G-quadruplex formation within the GDNA. The combined results of fluorescence and CD spectroscopy indicate that the proposed FRET-based methodology serves as a cost-effective, facile, and efficient tool for screening G-quadruplex ligands. This approach has significant potential for application in the identification of telomerase-targeting anticancer drugs.
SN - 2470-1343
ER -