Epigenetic Modulators as Therapeutic Agents in Cancer

Int J Mol Sci. 2023 Oct 6;24(19):14964. doi: 10.3390/ijms241914964.

Abstract

Epigenetics play a crucial role in gene regulation and cellular processes. Most importantly, its dysregulation can contribute to the development of tumors. Epigenetic modifications, such as DNA methylation and histone acetylation, are reversible processes that can be utilized as targets for therapeutic intervention. DNA methylation inhibitors disrupt DNA methylation patterns by inhibiting DNA methyltransferases. Such inhibitors can restore normal gene expression patterns, and they can be effective against various forms of cancer. Histone deacetylase inhibitors increase histone acetylation levels, leading to altered gene expressions. Like DNA methylation inhibitors, histone methyltransferase inhibitors target molecules involved in histone methylation. Bromodomain and extra-terminal domain inhibitors target proteins involved in gene expression. They can be effective by inhibiting oncogene expression and inducing anti-proliferative effects seen in cancer. Understanding epigenetic modifications and utilizing epigenetic inhibitors will offer new possibilities for cancer research.

Keywords: DNA methylation; cancer; epigenetics.

Publication types

  • Review

MeSH terms

  • Acetylation
  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • DNA Methylation
  • Epigenesis, Genetic
  • Histone Deacetylase Inhibitors / pharmacology
  • Histone Deacetylase Inhibitors / therapeutic use
  • Histones / metabolism
  • Humans
  • Neoplasms* / drug therapy
  • Neoplasms* / genetics

Substances

  • Histones
  • Antineoplastic Agents
  • Histone Deacetylase Inhibitors

Grants and funding

This research received no external funding.