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 demethylases are epigenetic erasers that remove the -CH3 group from lysine or arginine residues of histone proteins, altering the transcriptional activity and regulating chromatin state.

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Types of: HDMi
Drug Name FDA status
Pargyline
Clorgyline
Bizine
GSK2879552
KDM5-C70
JIB-04
Tranylcypromine
Phenelzine
ORY-1001
SID 85736331
Namoline
CBB1007
Methylstat
GSKJ4
GSKJ1
QC6352
SP2509
KDOAM-25
T-448
Daminozide
CPI-455
NCGC00244536
NCGC00247743
GSK-J2
Corin
GSK690
PBIT
S 2101
T-3775440 hydrochloride
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FDA Approved
FDA Approved
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