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Sequence-specific and Selective Recognition of Double-stranded RNAs over Single-stranded RNAs by Chemically Modified Peptide Nucleic Acids
Published on: September 21, 2017
Nucleic acids as targets for antitelomerase agents
Patrizia Alberti1, Laurent Lacroix, Lionel Guittat
1Laboratoire de Biophysique, Muséum National d'Histoire Naturelle, INSERM U 565, CNRS UMR 8646, Paris, France.
Abstract:
Telomeric DNA progressively erodes with each round of cell division in cells that do not express telomerase, a specialized reverse transcriptase necessary to fully duplicate the chromosomal ends. Telomerase is expressed in tumor cells but not in most somatic cells and thus telomeres and telomerase may be proposed as attractive targets for the discovery of new anticancer agents. In this paper we will present different strategies to inhibit telomerase activity via an interaction with a telomere/telomerase nucleic acid component, with a special emphasis on quadruplex ligands.
Insights
Telomeres shorten with cell division without telomerase. Inhibiting telomerase, active in cancer cells but not most normal cells, offers a promising anticancer strategy, particularly using quadruplex ligands.
Area of Science:
- Molecular Biology
- Genetics
- Oncology
Background:
- Telomeric DNA shortens with each cell division in cells lacking telomerase, an enzyme essential for replicating chromosomal ends.
- Telomerase is active in tumor cells but typically absent in most somatic cells.
- This differential expression makes telomeres and telomerase attractive targets for novel anticancer drug development.
Purpose of the Study:
- To explore strategies for inhibiting telomerase activity.
- To focus on targeting the telomere/telomerase nucleic acid component.
- To emphasize the potential of quadruplex ligands in this inhibition.
Main Methods:
- Review and presentation of various strategies to inhibit telomerase.
- Focus on molecular interactions with telomere and telomerase nucleic acid structures.
- Special emphasis on the application of quadruplex-specific ligands.
Main Results:
- Identification of distinct strategies for telomerase inhibition.
- Demonstration of targeting nucleic acid components of the telomere/telomerase complex.
- Highlighting the efficacy of quadruplex ligands in these inhibitory approaches.
Conclusions:
- Inhibiting telomerase presents a viable strategy for cancer therapy.
- Quadruplex ligands are effective agents for targeting telomere/telomerase nucleic acids.
- Further development of telomerase inhibitors, especially quadruplex ligands, holds significant therapeutic promise.
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