Target intelligence / Profile preview

Epigenetic regulators

Molecular classification
Enzyme, Transcription factor, Histone modification, DNA methyltransferase, Histone acetyltransferase, Histone deacetylase, Histone methyltransferase, Histone demethylase, Chromatin remodeler, Bromodomain-containing protein, Non-coding RNA
01

Overview

Epigenetic regulators are a diverse group of proteins and non-coding RNAs that control gene expression without altering the underlying DNA sequence [1, 11]. They are typically categorized into "writers" that add chemical groups to DNA or histones, "erasers" that remove these groups, and "readers" that recognize and bind to these modifications [1, 12]. These regulators play critical roles in normal development, cellular differentiation, and the maintenance of specific gene expression patterns across cell generations [1, 11]. Dysregulation of epigenetic processes is a hallmark of many diseases, particularly cancer, where it can lead to the silencing of tumor suppressor genes or the activation of oncogenes [3, 8]. Consequently, epigenetic regulators have become significant therapeutic targets in modern medicine [4, 5]. Several inhibitors targeting DNA methyltransferases and histone deacetylases are already FDA-approved for treating various hematologic malignancies [12, 14]. Ongoing research continues to explore their potential in solid tumors, neurodegenerative diseases, and metabolic disorders [2, 7, 12].

Other names
Epigenetic modifiersChromatin regulatorsEpigenetic proteinsEpigenetic machineryEpigenetic factors
02

Mechanism of action

Inhibition of DNA methyltransferases (DNMTs), histone deacetylases (HDACs), histone methyltransferases (HMTs), and bromodomain and extra-terminal (BET) proteins to restore normal gene expression patterns [5, 12, 14].

03

Biological functions

Gene expression regulationChromatin remodelingDNA methylationHistone modificationCell differentiationDevelopmentDNA repairCell cycle regulationApoptosis
04

Disease associations

CancerNeurodegenerative diseaseCardiovascular diseaseAutoimmune diseaseMetabolic disorderInfection
05

Safety considerations

Off-target effectsGlobal epigenetic changesHematologic toxicityGastrointestinal toxicityPotential for secondary malignanciesTransgenerational effects
06

Interacting drugs

Azacitidine

8 more in the full profile.

07

Biomarkers

DNA methylation patternsHistone acetylation levelsEZH2 mutationIDH1 mutationIDH2 mutationMGMT promoter methylation

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