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Published on: May 16, 2020
Tetraplex binding molecules as anti-cancer agents
Kevin M Doherty1, Sudha Sharma, Rigu Gupta
1Laboratory of Molecular Gerontology, National Institute on Aging, NIH, 5600 Nathan Shock Drive, Baltimore, MD 21224, USA.
Abstract:
Increasing evidence suggests that four-stranded tetraplex structures spontaneously form under physiological conditions and these alternate DNA structures are likely to form in vivo. Alternate G-quadruplex DNA structures that may form in regulatory elements of oncogenes or G-rich telomere sequences are potential targets for cancer therapy since these sequence-specific structures are proposed to affect gene expression and telomerase activation, respectively. Small molecule compounds that specifically bind tetraplexes may be used to regulate cell cycle progression by modulating promotor activation or disrupting telomere maintenance, important processes of cellular transformation. In this review, we summarize the current research developments and associated patents that bear relevance to understanding the mechanism and clinical application of tetraplex binding molecules as anti-cancer agents.
Insights
Four-stranded DNA structures, like G-quadruplexes, are forming in vivo and are promising cancer therapy targets. Small molecules binding these structures may offer new anti-cancer treatments by regulating gene expression and telomere maintenance.
Area of Science:
- Biochemistry
- Molecular Biology
- Genetics
Background:
- Four-stranded DNA structures, known as tetraplexes, are increasingly found to form under physiological conditions.
- G-quadruplex DNA structures are particularly relevant, potentially forming in oncogene regulatory elements and telomere sequences.
- These structures are implicated in critical cellular processes like gene expression and telomerase activation.
Purpose of the Study:
- To review current research on tetraplex binding molecules as potential anti-cancer agents.
- To explore the mechanisms by which these molecules interact with G-quadruplex DNA.
- To summarize relevant patent developments in this therapeutic area.
Main Methods:
- Literature review of scientific publications.
- Analysis of patent databases for tetraplex-targeting compounds.
- Synthesis of information on G-quadruplex structure and function.
Main Results:
- Tetraplexes are viable targets for therapeutic intervention in cancer.
- Small molecules that specifically bind tetraplexes show potential for modulating gene expression and telomere maintenance.
- Research and patent activity indicate growing interest in tetraplex-binding agents for cancer therapy.
Conclusions:
- Tetraplex binding molecules represent a promising class of anti-cancer agents.
- Targeting G-quadruplex structures offers novel strategies for cancer treatment.
- Further research and development of these molecules are warranted for clinical application.
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