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Updated: Jan 25, 2026
08:52
Chemical Dimerization-Induced Protein Condensates on Telomeres
Published on: April 12, 2021
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Cyclic Naphthalene Diimide Dimer with a Strengthened Ability to Stabilize Dimeric G-Quadruplex
Ryusuke Takeuchi1, Tingting Zou1,2, Daiki Wakahara1
1Department of Applied Chemistry, Kyushu Institute of Technology, Fukuoka, 804-8550, Japan.
Chemistry (Weinheim an Der Bergstrasse, Germany)
|May 10, 2019
Summary
New dimeric cyclic naphthalene diimide derivatives (cNDI-dimers) effectively stabilize dimeric G-quadruplex structures. These compounds show enhanced inhibition of telomerase activity, indicating improved anticancer potential for therapeutic applications.
Area of Science:
- Medicinal Chemistry
- Supramolecular Chemistry
- Biochemistry
Background:
- G-quadruplexes are four-stranded DNA structures implicated in various cellular processes, including telomere maintenance.
- Dysregulation of G-quadruplexes is linked to diseases like cancer, making them attractive therapeutic targets.
- Small molecules capable of selectively binding and stabilizing G-quadruplexes are sought for drug development.
Purpose of the Study:
- To design and synthesize novel dimeric cyclic naphthalene diimide derivatives (cNDI-dimers) with varying linker lengths.
- To investigate the binding affinity and selectivity of cNDI-dimers towards dimeric G-quadruplex structures.
- To evaluate the potential of cNDI-dimers as therapeutic agents by assessing their impact on telomerase activity and telomere elongation.
Main Methods:
- Chemical synthesis of cNDI-dimers with diverse linker lengths.
- Spectroscopic and biophysical techniques to assess G-quadruplex binding and stabilization.
- Enzyme inhibition assays to measure telomerase activity.
- Telomere DNA elongation assays.
Main Results:
- All synthesized cNDI-dimers demonstrated a high preference for G-quadruplex structures.
- cNDI-dimers significantly enhanced the thermal stability of dimeric G-quadruplexes, increasing melting temperature by over 23°C compared to monomers.
- cNDI dimers exhibited superior inhibition of telomerase activity and telomere DNA elongation compared to cNDI monomers.
Conclusions:
- Dimeric cyclic naphthalene diimide derivatives are effective binders and stabilizers of dimeric G-quadruplex structures.
- The enhanced stabilization and inhibitory properties of cNDI-dimers suggest significant potential for anticancer therapeutic applications.
- Further development of cNDI-dimers could lead to novel strategies for targeting telomerase and treating cancer.
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