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Related Experiment Video

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Targeting EHMT2/ G9a for cancer therapy: Progress and perspective.

Suraya Jan1, Mohd Ishaq Dar1, Rubiada Wani1

  • 1CSIR, Indian Institute of Integrative Medicine, Sanatnagar, 190005, Srinagar, Kashmir, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India.

European Journal of Pharmacology
|December 21, 2020
PubMed
Summary

Euchromatic histone lysine methyltransferase-2 (G9a) is crucial for gene regulation and development. Inhibiting G9a shows promise in cancer therapy by reducing cell growth and inducing cell death.

Keywords:
BIX-01294EHMT2EpigeneticsG9aH3K9me2SET domain

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Area of Science:

  • Epigenetics
  • Molecular Biology
  • Cancer Research

Background:

  • G9a (euchromatic histone lysine methyltransferase-2) is a key enzyme in heterochromatin formation and transcriptional repression.
  • It plays vital roles in development, cellular processes, and is implicated in various cancers.

Purpose of the Study:

  • To review the structure, biological activity, and targeting strategies for G9a.
  • To explore G9a's role in cancer and evaluate inhibitors for therapeutic development.

Main Methods:

  • Comprehensive literature search of databases (PubMed, Scopus) and clinical trials.
  • Systematic presentation of findings from cited papers.
  • Chemical structures drawn using Chemdraw.

Main Results:

  • G9a mediates histone H3K9 methylation, influencing gene expression.
  • Elevated G9a levels correlate with increased tumor growth and metastasis.
  • G9a inhibition reduces cancer cell proliferation and induces apoptosis, autophagy, and senescence.

Conclusions:

  • Targeting G9a presents a promising therapeutic strategy for various cancers.
  • Further research is needed to develop novel G9a inhibitors and treatment strategies.