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Updated: May 1, 2026

Author Spotlight: Advanced Single-Molecule Techniques for Investigating Telomeric Protein-DNA Interactions
Published on: August 30, 2024
Advances in the molecular design of potential anticancer agents via targeting of human telomeric DNA
Basudeb Maji1, Santanu Bhattacharya
1Department of Organic Chemistry, Indian Institute of Science, Bangalore-560012, India. sb@orgchem.iisc.ernet.in.
Abstract:
Telomerases are an attractive drug target to develop new generation drugs against cancer. A telomere appears from the chromosomal termini and protects it from double-stranded DNA degradation. A short telomere promotes genomic instability, like end-to-end fusion and regulates the over-expression of the telomere repairing enzyme, telomerase. The telomerase maintains the telomere length, which may lead to genetically abnormal situations, leading to cancer. Thus, the design and synthesis of an efficient telomerase inhibitor is a viable strategy toward anticancer drugs development. Accordingly, small molecule induced stabilization of the G-quadruplex structure, formed by the human telomeric DNA, is an area of contemporary scientific art. Several such compounds efficiently stabilize the G-quadruplex forms of nucleic acids, which often leads to telomerase inhibition. This Feature article presents the discovery and development of the telomere structure, function and evolution in telomere targeted anticancer drug design and incorporates the recent advances in this area, in addition to discussing the advantages and disadvantages in the methods, and prospects for the future.
Insights
Telomerase is a key target for new cancer drugs. Inhibiting telomerase by stabilizing G-quadruplex DNA structures offers a promising strategy for developing novel anticancer therapies.
Area of Science:
- Biochemistry
- Genetics
- Pharmacology
Background:
- Telomeres protect chromosomal ends from degradation.
- Shortened telomeres can cause genomic instability and cancer.
- Telomerase maintains telomere length, potentially driving cancer progression.
Purpose of the Study:
- To explore telomere structure, function, and evolution in anticancer drug design.
- To review recent advances in telomere-targeted drug development.
- To discuss the advantages and disadvantages of current methods.
Main Methods:
- Focus on small molecule-induced stabilization of G-quadruplex structures.
- Investigating compounds that stabilize human telomeric DNA G-quadruplexes.
- Reviewing literature on telomere-targeted anticancer drug design.
Main Results:
- Telomerase inhibitors are a viable strategy for anticancer drug development.
- Stabilization of G-quadruplex structures can lead to telomerase inhibition.
- Several compounds demonstrate efficacy in stabilizing G-quadruplex forms.
Conclusions:
- Telomere-targeted drug design, particularly G-quadruplex stabilization, is a promising area for cancer therapy.
- Further research is needed to optimize methods and overcome challenges.
- Future prospects involve developing efficient telomerase inhibitors for novel anticancer drugs.
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