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


HDACs act as erasers in epigenetic programming. Histone deacetylation is an important gene regulation process in which an acetyl group is removed from N-terminal ends of lysine residues from protruding tails of histone proteins from the core of nuclesomes making it more compact so as not to abide any interaction between DNA and other transcriptionary proteins . There are a total of four classes that categorize Histone Deacetylases (HDACs). Class I includes HDACs 1, 2, 3, and 8. Class II is divided into two subgroups, Class IIA and Class IIB. Class IIA includes HDACs 4, 5, 7, and 9 while Class IIB includes HDACs 6 and 10. Class III contains the Sirtuins and Class IV contains only HDAC11. Change in the pool of HDACs has been many times correlated with many neurological disorders, cancers. Thus study of HDAC inhibitors is developing rapidly.

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Types of: HDACi
Drug Name FDA status
Vorinostat
Givinostat
Panobinostat
AR-42
Entinostat
Apicidin
Pracinostat
Abexinostat
Resminostat
CUDC-101
Nicotinamide
Toxoflavin
Inauhzin
Cambinol
Salermide
Trichostatin A
Belinostat
CG-1521
Romidepsin
Valproic acid
OSU-HDAC-42
HC-toxin
Magnesium valproate
Plitidepsin
Tasquinimod
Sodium butyrate
Mocetinostat
Carbamazepine
Tefinostat
CHR-3996
Curcumin
QUISINOSTAT
Sodium phenylbutyrate
Pivanex
Butyroyloxymethyl-diethyl phosphate
Resveratrol
Dacinostat
Droxinostat
Psammaplin A
ITF-A
ITF-B
OSU-HDAC-44
Ricolinostat
Tubastatin A
RGFP966
TMP195
Fimepinostat
LMK-235
ACY-738
PCI-34051
Nexturastat A
CAY10603
ACY-775
WT-161
MC1568
RGFP109
Citarinostat
Scriptaid
Tucidinostat
Santacruzamate A
EDO-S101
Oxamflatin
HPOB
BML-210
Pomiferin
Domatinostat
BG45
Bufexamac
Sinapinic acid
FT895
CHDI-390576
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