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Targeting Epigenetics in Cancer.

Richard L Bennett1, Jonathan D Licht1

  • 1Division of Hematology & Oncology, Department of Medicine, University of Florida Health Cancer Center, University of Florida, Gainesville, Florida 32606, USA;

Annual Review of Pharmacology and Toxicology
|October 10, 2017
PubMed
Summary
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Cancer cells hijack epigenetic regulators, altering gene expression. Reversible epigenetic therapies offer promising new treatments for various cancers, targeting these key mechanisms.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Epigenetic alterations are key drivers in cancer development.
  • These changes affect DNA methylation, histone modifications, and chromatin structure.
  • Dysregulation disrupts normal gene expression patterns.

Purpose of the Study:

  • To review the role of epigenetic regulators in cancer.
  • To summarize the development of epigenetic therapies.
  • To discuss targeting epigenetic writers, readers, and erasers.

Main Methods:

  • Literature review of epigenetic mechanisms in cancer.
  • Analysis of current small molecule inhibitors targeting epigenetic regulators.
  • Summary of ongoing clinical trials.
Keywords:
DNA methylationanticancer therapiesepigenetic readersepigeneticshistone acetylationhistone methylation

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Main Results:

  • Epigenetic regulators are frequently dysregulated in cancer.
  • Small molecule inhibitors targeting epigenetic processes show promise.
  • Clinical trials are underway for hematologic malignancies and solid tumors.

Conclusions:

  • Epigenetic alterations are crucial in cancer.
  • Targeting epigenetic mechanisms represents a promising therapeutic strategy.
  • Reversible epigenetic therapies are advancing cancer treatment.