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Modulation of epigenetic targets for anticancer therapy: clinicopathological relevance, structural data and drug

Federico Andreoli1, Arménio Jorge Moura Barbosa, Marco Daniele Parenti

  • 1Department of Experimental Pathology, Alma Mater Studiorum - University of Bologna, Via S.Giacomo 14, 40126 Bologna, Italy.

Current Pharmaceutical Design
|September 29, 2012
PubMed

Insights

This review explores small-molecule inhibitors targeting cancer epigenetics. It highlights key epigenetic targets and their potential in developing new anticancer therapies.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • Cancer epigenetics research has advanced significantly.
  • Epigenetic alterations are crucial in cancer development and progression.
  • Epigenetic modifications regulate gene expression in cancer.

Purpose of the Study:

  • To provide an overview of small-molecule applications in cancer epigenetics.
  • To discuss current epigenetic targets for cancer therapy.
  • To review structural data and drug design perspectives for epigenetic targets.

Main Methods:

  • Literature review of epigenetic targets and small-molecule inhibitors.
  • Analysis of pre-clinical and clinical outcomes of epidrugs.
  • Examination of structural data for drug design insights.

Main Results:

  • Several epigenetic targets, including histone deacetylases and DNA methyltransferases, are identified.
  • Small-molecule inhibitors targeting these enzymes show pre-clinical and clinical promise.
  • Emerging targets involve enzymes modifying histone tails.

Conclusions:

  • Small molecules targeting epigenetic enzymes represent a promising area for cancer therapy.
  • Further research into structural data and drug design can accelerate the development of novel epidrugs.
  • The field of cancer epigenetics is rapidly evolving with new therapeutic opportunities.

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