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Targeting epigenetic regulations in cancer

Bo Ning1, Wenyuan Li2, Wei Zhao1

  • 1Center for Inflammation and Epigenetics, Houston Methodist Research Institute, Houston, TX 77030, USA.

Acta Biochimica Et Biophysica Sinica
|October 29, 2015
PubMed

Insights

Epigenetic regulation controls gene expression via DNA methylation and histone modifications. Targeting these epigenetic mechanisms shows promise for cancer therapy and disease treatment.

Area of Science:

  • Molecular Biology
  • Genetics
  • Epigenetics

Background:

  • Epigenetic regulation, including DNA methylation and histone modifications, dynamically controls gene expression.
  • These regulatory mechanisms are crucial in stem cell biology, development, and tumor genesis.
  • Aberrant epigenetic regulation is linked to various diseases, notably cancer.

Purpose of the Study:

  • To review key proteins involved in epigenetic regulation via DNA methylation, histone acetylation, and histone methylation.
  • To discuss the role of reader proteins that bind to modified histones.
  • To explore the association of these epigenetic factors with cancer and recent pharmacological developments.

Main Methods:

  • Literature review of studies on epigenetic regulatory proteins.
  • Analysis of proteins mediating DNA methylation and histone modifications.
  • Examination of reader proteins interacting with modified histones.
  • Review of cancer associations and drug development targeting epigenetic proteins.

Main Results:

  • Identified key proteins mediating DNA methylation, histone acetylation, and histone methylation.
  • Highlighted the function of reader proteins in interpreting epigenetic marks.
  • Demonstrated the significant association between epigenetic dysregulation and cancer development.
  • Summarized progress in developing drugs targeting epigenetic modifications for cancer therapy.

Conclusions:

  • Epigenetic regulation is a complex network involving DNA methylation, histone modifications, and reader proteins.
  • Abnormal epigenetic regulation is a hallmark of diseases, particularly cancer.
  • Targeting epigenetic mechanisms offers promising therapeutic strategies for cancer and other diseases.
Keywords:
DNA methylationanti-cancer drugsepigenetic regulationhistone modificationinhibitors

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