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Small-molecular modulators of cancer-associated epigenetic mechanisms

Yukihiro Itoh1, Takayoshi Suzuki, Naoki Miyata

  • 1Graduate School of Medical Science, Kyoto Prefectural University of Medicine, Taishogun, Kyoto 603-8334, Japan.

Molecular Biosystems
|March 21, 2013
PubMed

Insights

Epigenetic mechanisms like DNA methylation and histone modification control gene expression and cellular functions. Aberrations in these epigenetic processes are linked to cancer, and small molecules targeting them are used in therapy.

Area of Science:

  • Molecular Biology
  • Genetics
  • Cancer Research

Background:

  • Epigenetic mechanisms, including DNA methylation and histone modifications, regulate gene expression without altering DNA sequence.
  • These mechanisms are crucial for cellular functions like cell cycle control, immune responses, and signal transduction.
  • Epigenetic aberrations are implicated in oncogenesis and cancer cell proliferation, with alterations found in numerous human cancers.

Purpose of the Study:

  • To review chemical epigenetics in the context of cancer therapy.
  • To focus on small molecules that modulate epigenetic mechanisms relevant to cancer treatment.

Main Methods:

  • Literature review of chemical-biological approaches and small molecules.
  • Analysis of epigenetic mechanisms (DNA methylation, histone modification) in cancer.

Main Results:

  • Epigenetic dysregulation is closely linked to cancer development.
  • Several small molecules targeting epigenetic mechanisms have been approved for cancer therapy.
  • Small molecules modulating DNA methylation and histone modification are key therapeutic agents.

Conclusions:

  • Chemical epigenetics offers promising avenues for cancer therapy.
  • Targeting DNA methylation and histone modification with small molecules is a validated strategy in oncology.
  • Further research into chemical epigenetics can lead to novel cancer treatments.

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