Epigenetics refers to the study of heritable changes in gene function that are mediated by mechanisms other than nucleotide alterations in the primary DNA sequence. These changes are achieved by methylation on cytosine bases in DNA, by post-transcriptional modifications (e.g., acetylation and methylation) on histone proteins or RNA transcripts by non-coding RNAs (RNA-mediated gene silencing) [,,]. Nowadays, it is well established that the disruption of epigenetic processes plays a significant role in every step of carcinogenesis by altering gene expression profiles and protein functions. These global changes in the epigenetic landscape represent a hallmark of cancer [,,,]. The potential reversibility of epigenetic abnormalities encouraged the development of pharmacological modulators, so-called epigenetic drugs, against the writers, eraser or readers of epigenetics marks as valuable anti-cancer therapeutic targets. Although epigenetic drugs have a relevant therapeutic potential, only a relatively limited number of molecules including DNA methyltransferase (DNMT) and histone deacetylase (HDAC) inhibitors have been approved by the FDA and the EMEA for cancer treatment. Accordingly, there is an urgent need to develop new epigenetically active compounds for improved therapeutics in cancer therapy. Owing to their diverse biological activities and medicinal potentials, bioactive compounds isolated from natural sources (plants, fungi, marine life forms) and their derivatives, thanks to combinatorial chemistry, represent an inexhaustible source for drug discovery leading the development of new epigenetic drug candidates [,,,,,,]. In this presentation, we will focus on the significant findings regarding our research related to the characterization of new epigenetically active compounds of natural origin or their derivatives with anti-cancer activities.
Funding
ML and CF were supported by a grant from Télévie Luxembourg. This research is supported by the “Recherche Cancer et Sang” foundation, “Recherches Scientifiques Luxembourg” association, “Een Häerz fir kriibskrank Kanner” association, Action LIONS “Vaincre le Cancer” association and Télévie Luxembourg. This research is also supported by National Research Foundation (NRF) [grant number 019R1A2C1009231] and by a grant from the MEST of Korea for Tumor Microenvironment Global Core Research Center (GCRC) [grant number 2011-0030001]. Support from Brain Korea (BK21) PLUS program and Creative-Pioneering Researchers Program at Seoul National University [Funding number: 370C-20160062] are acknowledged. This article is based upon work from COST Action NutRedOx-CA16112 supported by COST (European Cooperation in Science and Technology).
Conflicts of Interest
The authors declare no conflict of interest.
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