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Updated: Jul 2, 2025
Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
Published on: August 5, 2022
Natural bioactive compounds targeting DNA methyltransferase enzymes in cancer: Mechanisms insights and efficiencies
Tarik Aanniz1, Abdelhakim Bouyahya2, Abdelaali Balahbib3
1Medical Biotechnology Laboratory, Rabat Medical & Pharmacy School, Mohammed V University in Rabat, Rabat, B.P, 6203, Morocco.
Abstract:
The regulation of gene expression is fundamental to health and life and is essentially carried out at the promoter region of the DNA of each gene. Depending on the molecular context, this region may be accessible or non-accessible (possibility of integration of RNA polymerase or not at this region). Among enzymes that control this process, DNA methyltransferase enzymes (DNMTs), are responsible for DNA demethylation at the CpG islands, particularly at the promoter regions, to regulate transcription. The aberrant activity of these enzymes, i.e. their abnormal expression or activity, can result in the repression or overactivation of gene expression. Consequently, this can generate cellular dysregulation leading to instability and tumor development. Several reports highlighted the involvement of DNMTs in human cancers. The inhibition or activation of DNMTs is a promising therapeutic approach in many human cancers. In the present work, we provide a comprehensive and critical summary of natural bioactive molecules as primary inhibitors of DNMTs in human cancers. The active compounds hold the potential to be developed as anti-cancer epidrugs targeting DNMTs.
Insights
Natural compounds can inhibit DNA methyltransferase enzymes (DNMTs), which are crucial for gene expression regulation. Targeting DNMTs with these molecules offers a promising strategy for developing novel anti-cancer epidrugs.
Area of Science:
- Molecular Biology
- Epigenetics
- Cancer Research
Background:
- Gene expression regulation is vital for cellular function and primarily occurs at DNA promoter regions.
- DNA methyltransferase enzymes (DNMTs) control DNA demethylation at CpG islands, influencing gene transcription.
- Aberrant DNMT activity is linked to cellular dysregulation, instability, and tumor development in human cancers.
Purpose of the Study:
- To comprehensively summarize natural bioactive molecules that inhibit DNMTs in the context of human cancers.
- To explore the potential of these natural compounds as anti-cancer epidrugs targeting DNMTs.
Main Methods:
- Literature review of natural bioactive molecules with DNMT inhibitory properties.
- Critical analysis of reported studies on DNMTs in human cancer.
- Evaluation of the therapeutic potential of identified compounds as epidrugs.
Main Results:
- Several natural bioactive molecules have been identified as primary inhibitors of DNMTs.
- These compounds demonstrate potential for modulating aberrant gene expression in cancer.
- The identified molecules represent promising candidates for anti-cancer drug development.
Conclusions:
- Natural compounds offer a viable source for developing DNMT inhibitors.
- Targeting DNMTs with natural bioactive molecules is a promising therapeutic avenue for human cancers.
- Further research into these compounds could lead to novel epidrugs for cancer treatment.
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