Pharmacological targeting of the cancer epigenome

Nat Cancer. 2024 Jun;5(6):844-865. doi: 10.1038/s43018-024-00777-2. Epub 2024 Jun 27.

Abstract

Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including disease initiation, maintenance and therapy resistance. As a result, there have been advances in the development and evaluation of epigenetic therapies for cancer, revealing substantial promise but also challenges. Three epigenetic inhibitor classes are approved in the USA, and many more are currently undergoing clinical investigation. In this Review, we discuss recent developments for each epigenetic drug class and their implications for therapy, as well as highlight new insights into the role of epigenetics in cancer.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • DNA Methylation / drug effects
  • Epigenesis, Genetic* / drug effects
  • Epigenome*
  • Gene Expression Regulation, Neoplastic / drug effects
  • Histone Deacetylase Inhibitors / pharmacology
  • Histone Deacetylase Inhibitors / therapeutic use
  • Humans
  • Molecular Targeted Therapy / methods
  • Neoplasms* / drug therapy
  • Neoplasms* / genetics

Substances

  • Antineoplastic Agents
  • Histone Deacetylase Inhibitors