Epigenetic Therapies and Potential Drugs for Treating Human Cancer

Curr Drug Targets. 2020;21(11):1068-1083. doi: 10.2174/1389450121666200325093104.

Abstract

Epigenetic modifications ensure the maintenance of normal cellular functions, and their dysregulation is frequently found in many disease states, including cancer. Nowadays, the most studied epigenetic dysregulation associated with tumorigenesis, cancer progression and metastasis refers to the variations in DNA methylation, histone modification and chromatin structure. The development of novel agents targeting these processes has enabled us to open up new pathways for anti-cancer strategies. To date, many small molecules have been designed to target epigenetic modifiers, and some of them are currently in clinical trials for patients with haematologic malignancies and solid tumours. With this in mind, we elaborate on basic information on epigenetic modifications and potential epigenetic therapies for cancer treatment.

Keywords: DNA methylation; Epigenetic; Histones; cancer; epigenetic drugs; therapies.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use*
  • DNA Methylation / drug effects
  • Drug Therapy, Combination / methods
  • Epigenesis, Genetic / drug effects*
  • Histones / metabolism
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / genetics*
  • Protein Processing, Post-Translational / drug effects

Substances

  • Antineoplastic Agents
  • Histones