Epigenetic Therapy Against Cancer: Toward New Molecular Targets and Technologies

Epigenetics is defined as a group of inheritable changes in gene expression without modifications to the DNA sequence. Examples of epigenetic control are DNA methylation, histone deacetylation and non-coding RNA expression. In the eukaryotic nucleus, DNA is compacted as chromatin by nucleosome units. Chemical modifications of histone proteins result in a distinct chromatin pattern through different epigenetic chromatin enzymatic and non-enzymatic modifiers. Chromatin remodeling complexes can be categorized as writers, which introduce several chemical modifications on DNA and histones; readers, proteins containing domains which are able to identify aforementioned modifications; and erasers, enzymes proficient in removing these chemical tags. Writers include DNA methyltransferases (DNMTs), histone lysine methyltransferases (KMTs), and histone acetyltransferases (HATs); readers include bromodomain proteins that read acetyl groups on histone lysine and methyl CpG binding domain (MDB); erasers include histone lysine demethylases and histone deacetylases.

Research on chromatin-remodeling complexes and their regulatory factors has been providing significant insights into diseases that affect humans, such as cancer. There is strong evidence for the relation between mutated and/or dysfunctional epigenomic chromatin modifiers and the development of different types of cancer. These epigenetic alterations could trigger the disruption of several molecular mechanisms that accelerate cancer progression and metastasis, including uncontrolled proliferative signals, cell death impairment, lesser tumor growth control, and angiogenesis promoting factors. The field of epigenetics is a modern research topic that offers promising therapeutic possibilities for chromatin regulation in cancer treatment, with new drugs being developed associated with innovative pharmacological and molecular approaches. Therefore, because of the above-mentioned reasons, studies involving epigenetic mechanisms could prove to be a way of developing successful therapies against cancer.

Areas to be covered in this Research Topic may include, but are not limited to:


• Design and synthesis of novel drugs for functional epigenetic anticancer therapy.
• Pharmacological and molecular anticancer therapies targeting histone-modifying molecules.
• Understanding of epigenetic targets and cancer cell signaling (cytoskeleton organization, apoptosis, autophagy, among others) in cancer therapy.
• Metabolic targets for the development of drugs against epigenetic-dependent cancers.
• Influence of epigenetic therapy on cancerous stem cells, cancer invasion/metastasis and viral infection-based cancer cells.
• Clinical studies and their significance in identifying epigenetic molecular targets for cancer treatment.
• Role of micro-organisms in cancer epigenetic regulation and interventional therapeutic strategies.
• Epigenetic studies landscape related to immune response and immunotherapy against cancer.
• Nanotechnology's role in the enhancement of therapeutic action against cancer.
• CRISPR-Cas9 systems in epigenome modulation and their applications in cancer therapy.
• Single-cell analysis as a tool to evaluate epigenetic molecular targets in cancer therapy.
• Interaction between coding and non-coding RNAs expression (miRNA, lncRNA, circRNA) and epigenetic modifiers as an approach for cancer therapy.