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Multitarget Drugs: an Epigenetic Epiphany.

A Ganesan1

  • 1School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich, NR4 7TJ, UK. a.ganesan@uea.ac.uk.

Chemmedchem
|February 19, 2016
PubMed
Summary

Epigenetic modifications regulate gene expression without altering DNA sequence. This review covers key epigenetic drug targets and their clinical progress, focusing on cancer treatments.

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Genetics

Background:

  • Epigenetics involves heritable changes in gene expression not caused by DNA sequence alterations.
  • Key epigenetic mechanisms include DNA methylation and histone modifications, orchestrated by specific enzymes.
  • Epigenetic dysregulation is implicated in various diseases, notably cancer, making epigenetic modifiers attractive therapeutic targets.

Purpose of the Study:

  • To review epigenetic targets that have advanced to clinical trials.
  • To survey drugs with multitarget mechanisms including epigenetic modulation.
  • To highlight the therapeutic potential of targeting epigenetic machinery in cancer.

Main Methods:

  • Literature review of epigenetic targets in clinical development.
  • Analysis of drug discovery efforts targeting epigenetic enzymes and recognition domains.
  • Survey of approved and investigational drugs with epigenetic mechanisms of action.

Main Results:

  • Several epigenetic targets, including DNA methyltransferases, histone deacetylases, lysine methyltransferases, lysine demethylases, and bromodomains, have reached clinical stages.
  • A growing number of multitarget drugs incorporate epigenetic modulation as a key therapeutic strategy.
  • These epigenetic drugs show promise for various cancers and other diseases.

Conclusions:

  • Epigenetic targets represent a rapidly advancing frontier in drug discovery, particularly for oncology.
  • Targeting epigenetic enzymes and recognition domains offers novel therapeutic avenues.
  • Multitarget drugs engaging epigenetic pathways hold significant potential for improved treatment outcomes.
Keywords:
cancerdual inhibitorsepigeneticshistone deacetylasesmultitarget drugs

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