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The Search for Potent, Small-Molecule HDACIs in Cancer Treatment: A Decade After Vorinostat

Chiara Zagni1, Giuseppe Floresta1,2, Giulia Monciino1

  • 1Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, Viale Andrea Doria 6, 95125, Catania, Italy.

Medicinal Research Reviews
|February 10, 2017
PubMed

Insights

Histone deacetylase inhibitors (HDACIs) target epigenetic changes in cancer. This review covers HDACI progress and mechanisms from 2011-2015, highlighting approved drugs for lymphoma.

Area of Science:

  • Epigenetics
  • Molecular Biology
  • Pharmacology

Background:

  • Histone deacetylases (HDACs) are key regulators of chromatin remodeling and gene expression.
  • HDAC inhibition is a promising strategy for treating cancers and other diseases.
  • Over 20 HDAC inhibitors (HDACIs) have entered clinical trials, with some approved for cutaneous T-cell lymphoma.

Purpose of the Study:

  • To provide an overview of current knowledge on HDACIs.
  • To summarize progress and molecular mechanisms of HDACIs.
  • To cover the period from 2011 to 2015.

Main Methods:

  • Literature review of scientific publications.
  • Analysis of clinical trial data.
  • Synthesis of information on HDAC inhibitor mechanisms.

Main Results:

  • Significant advancements in understanding HDAC biology and inhibitor development.
  • Clinical validation of HDACIs in specific cancer types.
  • Identification of key molecular pathways targeted by HDACIs.

Conclusions:

  • HDACIs represent a vital class of epigenetic drugs with therapeutic potential.
  • Continued research is crucial for expanding HDACI applications.
  • The period 2011-2015 marked substantial progress in the field of HDAC inhibition.
Keywords:
benzamidescyclic peptidesepigeneticshistone deacetylase inhibitorshydroxamic acids

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