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Design of small molecule epigenetic modulators.

Boobalan Pachaiyappan1, Patrick M Woster1

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Summary

Epigenetics, the study of gene expression changes without altering DNA sequence, offers new drug targets. Modulating epigenetic writers, erasers, and readers can treat diseases linked to epigenome aberrations.

Keywords:
AcetyllysineEpigeneticHistoneMethylarginineMethyllysine

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Area of Science:

  • Epigenetics and molecular biology.
  • Drug discovery and development.

Background:

  • Epigenetic mechanisms, including DNA methylation and histone modifications, regulate gene expression.
  • Aberrations in epigenetic regulation are implicated in various diseases.
  • The epigenome comprises functional elements categorized as writers, erasers, and readers.

Purpose of the Study:

  • To summarize the components of epigenetic control of gene expression.
  • To describe current efforts in identifying small molecules that modulate epigenetic processes for therapeutic purposes.

Main Methods:

  • Review of epigenetic machinery components (writers, erasers, readers).
  • Exploration of small molecule modulators targeting epigenetic processes.
  • Analysis of the role of epigenetics in cellular homeostasis and disease.

Main Results:

  • Epigenetic machinery components (writers, erasers, readers) are crucial for gene expression and cellular homeostasis.
  • Epigenomic aberrations are linked to diverse diseases.
  • Small molecules targeting epigenetic processes represent a promising therapeutic strategy.

Conclusions:

  • Targeting epigenetic mechanisms offers a viable approach for novel drug discovery.
  • Understanding epigenetic control is key to developing treatments for epigenome-related diseases.