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Updated: Aug 23, 2025

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
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Modulation of DNA/RNA Methylation by Small-Molecule Modulators and Their Implications in Cancer

Ayushi Verma1, Abhipsa Sinha1, Dipak Datta2

  • 1Division of Cancer Biology, CSIR-Central Drug Research Institute (CDRI), Lucknow, India.

Sub-Cellular Biochemistry
|October 27, 2022
PubMed

Insights

Small molecules targeting DNA and RNA methylation are crucial for cancer therapy. These epigenetic modulators regulate gene expression, offering new avenues for cancer drug discovery and treatment.

Area of Science:

  • Molecular Biology
  • Epigenetics
  • Cancer Research

Background:

  • Chromatin, a complex of DNA, histones, and RNA, undergoes modifications like DNA and RNA methylation.
  • Deregulation of chromatin methylation is linked to human diseases, particularly cancer, due to altered gene expression.
  • Cancer involves dynamic epigenetic changes, with DNA methyltransferases (DNMTs) and m6A RNA methylation playing key roles in tumor development.

Purpose of the Study:

  • To review the role of small-molecule modulators in regulating DNA and RNA methylation.
  • To discuss the implications of these modulators in cancer therapy and drug discovery.

Main Methods:

  • Focus on small-molecule modulators targeting epigenetic mechanisms.
  • Review of recent studies on chemical modulators of DNA/RNA methylation.

Main Results:

  • Several small-molecule modulators targeting DNA/RNA methylation have been identified.
  • Some modulators are approved for cancer therapy, while others are in clinical trials.

Conclusions:

  • Small-molecule modulators offer promising therapeutic strategies for cancer by targeting epigenetic alterations.
  • Targeting DNA/RNA methylation represents a significant area in current cancer drug discovery research.
Keywords:
DNA methylationDNMTsDrug discoveryEpigeneticsRNA methylationSmall-molecule modulator

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