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Updated: May 15, 2026

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
Published on: September 20, 2018
G9a, a multipotent regulator of gene expression.
Shilpa Rani Shankar1, Avinash G Bahirvani, Vinay Kumar Rao
1Department of Physiology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, Singapore.
The methyltransferase G9a, known for gene repression, also activates gene expression via novel mechanisms. Its complex roles in development and disease highlight its potential as a therapeutic target.
Area of Science:
- Molecular Biology
- Epigenetics
- Gene Regulation
Background:
- The enzyme G9a catalyzes lysine methylation, primarily linked to transcriptional repression.
- Emerging evidence reveals G9a's non-canonical roles in gene activation, independent of its methyltransferase function.
Purpose of the Study:
- To review the diverse molecular mechanisms and substrates involved in G9a-mediated gene regulation.
- To discuss the multifaceted roles of G9a in biological processes and disease.
Main Methods:
- Literature review of recent studies on G9a function.
- Analysis of molecular pathways and protein substrates regulated by G9a.
- Synthesis of evidence regarding G9a's involvement in development and disease.
Main Results:
- G9a regulates gene expression through both canonical repression and non-canonical activation pathways.
- G9a substrates include histones and non-histone proteins, influencing various cellular processes.
- G9a plays critical roles in cell development, pluripotency, differentiation, and cell cycle control.
Conclusions:
- G9a exhibits complex and context-dependent functions in gene regulation.
- Dysregulated G9a expression is implicated in various human pathologies, including cancer.
- G9a represents a promising therapeutic target for treating diverse diseases.
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