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


DNA methyltransferases are writer enzymes that transfer -CH3 group from SAM (S-Adenosyl methionin) molecules to the cytosine residues in the CpG islands of promoter regions of our genes. There are 3 major DNMTs: DNMT1, DNMT3a and DNMT3b. DNMT1 is a maintenance DNMT, while DNMT3a and 3b are de novo DNMTs.

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Types of: DNMTi
Drug Name FDA status
Decitabine
5-Azacytidine
Hydralazine
Procainamide
Epigallocatechin-3-gallate
Zebularine
Equol
Genistein
SGI-110
Procaine
Nanaomycin A
Disulfiram
Lomeguatrib
RG108
SGI-1027
MG98
CP-4200
Hinokitiol
DC_517
DC-05
FDA Approved
FDA Approved
FDA Approved
FDA Approved
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental