Epigenetic modifier

Epigenetic modifiers are a diverse group of proteins and enzymes that regulate gene expression by modifying the chemical structure of DNA and histones without altering the underlying genetic sequence [1.1.4, 1.2.1]. These modifiers are functionally categorized into "writers" that add chemical marks (e.g., DNA methyltransferases, histone acetyltransferases), "erasers" that remove them (e.g., histone deacetylases, lysine demethylases), and "readers" that recognize and bind to these marks (e.g., bromodomain-containing proteins) [1.1.4, 1.3.3]. Dysregulation of these processes is a hallmark of many diseases, particularly cancer, where aberrant epigenetic silencing of tumor suppressor genes or activation of oncogenes drives disease progression [1.1.3, 1.3.5]. Therapeutic agents targeting these modifiers, known as "epidrugs," aim to reverse these pathological states by restoring normal chromatin structure and gene expression profiles [1.1.4, 1.3.5]. While several inhibitors of DNA methyltransferases (DNMTs) and histone deacetylases (HDACs) are FDA-approved for hematologic malignancies, the field is expanding to include targets like EZH2 and IDH1/2, as well as applications in neurodegenerative and inflammatory diseases [1.1.5, 1.2.2].

Other names

Epigenetic regulatorsChromatin modifiersEpigenetic enzymesChromatin-modifying enzymesEpigenetic factors

Inhibition of enzymes responsible for adding, removing, or reading epigenetic marks on DNA and histones to restore normal gene expression patterns.