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


Histone methyltransferases are epigenetic writers that transfer -CH3 group from SAM (S- Adenosyl methionine) molecules to lysine (lysine specific HMTs) or arginine (arginine specific HMTs) residues of N-terminal tails of histone proteins.

Search:
Types of: HMTi
Drug Name FDA status
UNC0321
UNC0224
EPZ-6438
DZNep
GSK343
Chaetocin
BIX-01338
BIX-01294
UNC0638
EPZ005687
GSK126
EPZ-5676
EPZ004777
SGC0946
E72
A-366
UNC1999
CPI360
UNC0965
BIX-01337
EI1
GSK503
BCI-121
LLY-507
EPZ015666
AZ505 ditrifluoroacetate
GSK3326595
MS023
UNC0642
JNJ-64619178
CM-579
EED226
MI-503
EPZ015866
MI-463
MI-538
MS049
CPI-169
BRD9539
LLY-283
EML741
OTS186935
SGC3027
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