Uncovering epigenetic landscape: a new path for biomarkers identification and drug development

Mol Biol Rep. 2020 Nov;47(11):9097-9122. doi: 10.1007/s11033-020-05916-3. Epub 2020 Oct 21.

Abstract

Scientific advances in recent decades have revealed an incredible degree of plasticity in gene expression in response to various environmental, nutritional, physiological, pathological, and behavioral conditions. Epigenetics emerges in this sense, as the link between the internal (genetic) and external (environmental) factors underlying the expression of the phenotype. Methylation of DNA and histone post-translationa modifications are canonical epigenetic events. Additionally, noncoding RNAs molecules (microRNAs and lncRNAs) have also been proposed as another layer of epigenetic regulation. Together, these events are responsible for regulating gene expression throughout life, controlling cellular fate in both normal and pathological development. Despite being a relatively recent science, epigenetics has been arousing the interest of researchers from different segments of the life sciences and the general public. This review highlights the recent advances in the characterization of the epigenetic events and points promising use of these brands for the diagnosis, prognosis, and therapy of diseases. We also present several classes of epigenetic modifying compounds with therapeutic applications (so-call epidrugs) and their current status in clinical trials and approved by the FDA. In summary, hopefully, we provide the reader with theoretical bases for a better understanding of the epigenetic mechanisms and of the promising application of these marks and events in the medical clinic.

Keywords: Biomarkers; Clinical Trials; DNA Methylation; Epidrugs; Histone Post-translational Modifications; Non-coding RNAs.

Publication types

  • Review

MeSH terms

  • Animals
  • Biomarkers / metabolism*
  • DNA Methylation*
  • Drug Development / methods*
  • Epigenesis, Genetic*
  • Gene Expression Regulation
  • Histone Code*
  • Humans
  • MicroRNAs / genetics
  • RNA, Long Noncoding / genetics

Substances

  • Biomarkers
  • MicroRNAs
  • RNA, Long Noncoding