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Current limitations and future opportunities for epigenetic therapies

F Cherblanc1, N Chapman-Rothe, R Brown

  • 1Imperial College London, South Kensington Campus, Department of Chemistry, London SW7 2AZ, UK.

Future Medicinal Chemistry
|March 16, 2012
PubMed

Insights

Epigenetic therapies offer new cancer treatment avenues by reversing aberrant gene expression. Histone lysine methyltransferases represent a promising, yet unexploited, therapeutic target for developing novel small-molecule inhibitors.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • Cancer is characterized by widespread epigenetic alterations affecting gene expression.
  • Epigenetic changes can be reversed using small-molecule inhibitors targeting epigenetic maintenance enzymes.
  • Current epigenetic drugs show efficacy in hematological cancers but limited success in solid tumors.

Purpose of the Study:

  • To review advancements in epigenetic cancer therapies.
  • To identify promising epigenetic targets for improved cancer treatment.
  • To discuss challenges and future directions in epigenetic therapy development.

Main Methods:

  • Review of current literature on epigenetic therapies and cancer.
  • Analysis of the role of epigenetic modifications in cancer hallmarks.
  • Examination of small-molecule inhibitors targeting epigenetic enzymes.
  • Discussion of crystallographic studies on histone lysine methyltransferases.

Main Results:

  • DNA-demethylating agents and histone deacetylase inhibitors demonstrate anti-tumor activity in certain hematological malignancies.
  • The efficacy of current epigenetic therapies in solid tumors remains uncertain.
  • Histone lysine methyltransferases are identified as a highly promising epigenetic target for cancer therapy.

Conclusions:

  • Epigenetic therapies hold potential for improving cancer treatment.
  • Challenges in drug delivery, pharmacodynamic response, and therapeutic index need to be addressed.
  • Histone lysine methyltransferases offer a novel target for developing effective small-molecule inhibitors for cancer treatment.

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