Introduction

Epigenetic changes such as DNA methylation and histone methylation and acetylation alter gene expression at the level of transcription by upregulating, downregulating, or silencing genes completely. Dysregulation of epigenetic events can be pathological, leading to cardiovascular disease, neurological disorders, metabolic disorders, and cancer development. Therefore, identifying drugs that inhibit these epigenetic changes are of great clinical interest. In our database we have the major classes of epigenetic drugs currently in use, such as DNA methylation inhibiting drugs, bromodomain inhibitors, histone acetyl transferase inhibitors, histone deacetylase inhibitors, protein methyltransferase inhibitors, and histone methylation inhibitors.

Source: Use of Epigenetic Drugs in Disease: An Overview, Sarah Heerboth et al.,2016


HATs are the writers of epigenetic programming. Histone acetylation is a process where an acetyl group is transferred to lysine residues at the N-terminal ends of protruding tails of histone proteins from the core of nucleosomes making it more accesible for the transcription factors to bind. Acetylation of histone proteins is a sign of transcriptional activation. Histone acetyltransferases are a large group of enzymes divided into many protein families like GNAT family(General Control Non-Derepressible 5 (Gcn5) –related N-Acetyltransferases (GNATs) , MOZ (Monocytic Leukemia Zinc Finger Protein), Ybf2/Sas3, Sas2 and Tip60 (Tat Interacting Protein) i.e. MYST, p300/CBP family (Adenoviral E1A-associated protein of 300kDa (p300) and the CREB-binding protein (CBP))

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Types of: HATi
Drug Name FDA status
Gallic acid
Garcinol
Anacardic acid
Procyanidin
MB-3
CTK7A
Plumbagin
Embelin
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental