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


Protein arginine deiminases (PADs), a unique family of enzymes that catalyzes citrulination i.e. that catalyzes the hydrolysis of peptidyl-arginine to form peptidyl-citrulline on histones, fibrinogen, and other biologically relevant proteins. PAD family is composed of five, calcium dependent isozymes (PADs 1–4 and 6) which are tissue specific. (Source: PMCID: PMC3507426)

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Types of: PADi
Drug Name FDA status
YW3-56
YW4-03
YW4-15
D-o-F-amidine
Cl-amidine
GSK484
Experimental
Experimental
Experimental
Experimental
Experimental
Experimental