article · Chemico-Biological Interactions
Gene expression regulation takes place primarily at gene promoter regions, determining accessibility for RNA polymerase. Enzymes known as DNA methyltransferases control this mechanism by acting at CpG islands to influence transcription. When these enzymes exhibit abnormal expression or activity, gene regulation fails, triggering cellular dysregulation, instability, and tumour development. Because of their documented involvement across human cancers, modifying DNA methyltransferase activity offers a viable route for oncology therapies. Natural bioactive molecules serve as primary inhibitors of these enzymes, demonstrating distinct mechanisms and efficiencies. These naturally derived compounds present opportunities for development into targeted anti-cancer epidrugs capable of modulating epigenetic enzyme function in cancer treatment.
Abnormal epigenetic regulation is a major driver of cancer development. Identifying natural compounds that inhibit DNA methyltransferases provides a foundation for designing targeted therapies, known as epidrugs. Understanding how these bioactive molecules influence gene expression allows researchers to explore treatments that can correct cellular dysfunction in various human cancers.
This work highlights natural bioactive compounds that could serve as starting points for anti-cancer epidrugs targeting DNA methyltransferase enzymes. Pharmaceutical developers and oncology researchers could use these findings to guide early lead discovery. Given that the abstract presents a summary of compound mechanisms and efficiencies, the research sits at an early exploratory stage, far from clinical application.
AI-generated from the published abstract. Always read the original work before citing.
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.
This page summarises published work. The authoritative version sits with the publisher.
DOI: 10.1016/j.cbi.2024.110907
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