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Writing and rewriting the epigenetic code of cancer cells: from engineered proteins to small molecules

Pilar Blancafort1, Jian Jin, Stephen Frye

  • 1School of Anatomy, Physiology, and Human Biology, M309, the University of Western Australia, 35 Stirling Highway, Crawley, 6009, WA, Australia. pilar.blancafort@uwa.edu.au

Molecular Pharmacology
|November 15, 2012
PubMed

Insights

The epigenomic era reveals molecular processes shaping chromatin. This review summarizes pharmacological strategies, including small molecule inhibitors and engineered proteins, to modify the cancer epigenome for therapeutic intervention.

Area of Science:

  • Epigenetics and Cancer Biology
  • Molecular Oncology

Background:

  • The epigenome, including methylomes, transcriptosomes, histone modifications, and noncoding RNAs, plays a crucial role in shaping the chromatin landscape.
  • Aberrant epigenetic processes are implicated in cancer development and progression.
  • Large-scale mapping of these epigenetic marks in cancer cells has identified novel therapeutic targets.

Purpose of the Study:

  • To summarize current pharmacological strategies for modifying the epigenetic landscape in cancer cells.
  • To highlight novel therapeutic opportunities arising from epigenomic research.

Main Methods:

  • Review of pharmacological approaches targeting epigenetic dysregulation in cancer.
  • Discussion of small molecule inhibitors of epigenetic enzymes.
  • Exploration of engineered proteins for epigenetic reprogramming.

Main Results:

  • Epigenetic modifications are key targets for anticancer therapies.
  • Small molecule inhibitors offer a strategy to correct aberrant epigenetic marks.
  • Engineered proteins show potential for stable epigenetic reprogramming.

Conclusions:

  • Pharmacological modulation of the epigenome represents a promising avenue for cancer treatment.
  • Targeting specific epigenetic alterations in cancer cells can lead to effective therapeutic interventions.
  • Future research should focus on developing precise and stable epigenetic reprogramming strategies.

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