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[Targeted epigenetic therapy of cancer. Achievements and perspectives]

Víctor Manuel Valdespino-Gómez1, Víctor Edmundo Valdespino-Castillo

  • 1Departamento de Atención a la Salud, Unidad Xochimilco, Universidad Autónoma Metropolitana, México D. F., México. vvaldespinog@yahoo.com.mx.

Cirugia Y Cirujanos
|January 29, 2013
PubMed

Insights

Epigenetic alterations in cancer, like DNA methylation changes and histone deacetylase activity, are key targets for new therapies. Epigenetic drugs aim to restore normal cell function and improve cancer treatment outcomes.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Epigenetic modifications, including DNA methylation and histone acetylation, play crucial roles in normal cellular function and are frequently dysregulated in cancer.
  • Aberrant epigenetic changes, such as promoter hypermethylation of tumor suppressor genes and global DNA hypomethylation, are hallmarks of cancer development.
  • Histone deacetylases (HDACs) are often overexpressed and highly active in cancer cells, contributing to the altered epigenetic landscape.

Purpose of the Study:

  • To review the physiological and pathophysiological epigenetic changes in normal and cancer cells.
  • To highlight the advancements and future directions in cancer epigenetic therapy.
  • To discuss the potential of epigenetic alterations as biomarkers for early detection, prognosis, and prediction in cancer.

Main Methods:

  • Review of existing literature on cancer epigenetics and epigenetic therapy.
  • Analysis of epigenetic targets, focusing on histone deacetylases (HDACs) and DNA methyltransferases (DNMTs).
  • Examination of approved epigenetic drugs and their therapeutic applications.

Main Results:

  • Epigenetic alterations are fundamental to cancer, involving DNA methylation and histone modifications.
  • Inhibition of HDACs and DNMTs represents a promising therapeutic strategy, with drugs like azacitidine, decitabine, vorinostat, and romidepsin already approved for certain hematological malignancies.
  • Epigenetic markers show significant potential for early cancer detection, prognosis, and predicting treatment response.

Conclusions:

  • Epigenetic therapy offers a novel approach to cancer treatment by aiming to reverse aberrant epigenetic modifications and restore normal cellular function.
  • Understanding cancer-specific epigenetic alterations provides new avenues for designing targeted and effective cancer therapies.
  • Future research should focus on developing more specific epigenetic drugs with reduced side effects to maximize therapeutic benefits.

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