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Epigenetic Modulators as Treatment Alternative to Diverse Types of Cancer

Jorseth Rodelo Gutiérrez1, Arturo René Mendoza Salgado1, Marcio De Ávila Arias2

  • 1Organic and Biomedical Chemistry Research Group, Faculty of Basic Sciences, Universidad del Atlántico, Barranquilla, Colombia.

Current Medicinal Chemistry
|December 29, 2021
PubMed

Insights

Chromatin, a complex of DNA and proteins, plays a key role in gene expression and cancer. This review explores epigenetic modifications in cancer and promising therapeutic inhibitors.

Area of Science:

  • Epigenetics and Molecular Biology
  • Cancer Research

Background:

  • DNA is packaged into chromatin, a complex of DNA and proteins.
  • Chromatin structure and its alterations are crucial for gene expression control.
  • Epigenetic mechanisms like DNA methylation and histone modifications are implicated in various cancers.

Purpose of the Study:

  • To review alterations in gene expression and epigenetic modification patterns in cancer cells.
  • To identify key modulators and inhibitors of epigenetic mechanisms in cancer.
  • To analyze the molecular evolution of representative epigenetic inhibitors.

Main Methods:

  • Literature review of epigenetic alterations in cancer.
  • Analysis of gene expression changes and epigenetic modification patterns.
  • Examination of modulators, inhibitors, and molecular evolution of epigenetic drugs.

Main Results:

  • Significant alterations in gene expression and epigenetic patterns are observed in cancer cells.
  • Several epigenetic mechanisms, including DNA methylation and histone modifications, are critical in cancer development.
  • Specific inhibitors targeting histone acetyltransferases (HAT), histone deacetylases (HDAC), DNA methyltransferases (DNMT), and chromatin remodelers show therapeutic potential.

Conclusions:

  • Epigenetic modifications are central to cancer pathogenesis.
  • Targeting epigenetic mechanisms offers a promising therapeutic strategy for cancer treatment.
  • The development of HAT, HDAC, DNMT, and domain inhibitors represents a significant advancement in cancer therapy.
Keywords:
CancerDNAchromatinepigenetic inhibitorepigenomahistone

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