Re-Sensitizing Tumor Cells to Cancer Drugs with Epigenetic Regulators

Curr Cancer Drug Targets. 2021;21(4):353-359. doi: 10.2174/1568009620666210108102723.


Cancer drug resistance is a major problem for cancer therapy. While many drugs can be effective in first-line treatments, cancer cells can become resistant due to genetic (mutations and chromosomal aberrations) but also epigenetic changes. Hence, many research studies addressed epigenetic drugs in circumventing resistance to conventional therapeutics in different tumor entities and in increasing the efficiency of immune checkpoint therapies. Furthermore, repositioning of already approved drugs in combination with epigenetic modifiers could potentiate their efficacy and thus could be an attractive strategy for cancer treatment. Summarizing, we recapitulate current data on epigenetic drugs and their targets in modulating sensitivity towards conventional and immune therapies, providing evidence that altering expression profiles by epigenetic modifiers holds great potential to improve the clinical outcome of cancer patients.

Keywords: Cancer drug resistance; DNA methylation; combinatorial treatments; epigenetic drugs; histone modification; re-sensitizing.

Publication types

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

MeSH terms

  • Antineoplastic Agents / classification
  • Antineoplastic Agents / pharmacology*
  • Drug Discovery
  • Drug Repositioning
  • Drug Resistance, Neoplasm / genetics*
  • Drug Therapy, Combination / methods
  • Drug Therapy, Combination / trends
  • Epigenesis, Genetic / drug effects*
  • Gene Expression Regulation, Neoplastic
  • Histone Code* / drug effects
  • Histone Code* / physiology
  • Humans
  • Neoplasms* / drug therapy
  • Neoplasms* / genetics
  • Neoplasms* / metabolism


  • Antineoplastic Agents