Target intelligence / Profile preview

Histone Deacetylase Class I (HDAC Class I)

Target
HDAC Class I
Molecular classification
Enzyme, Histone Modification Enzyme, Hydrolase
01

Overview

Histone deacetylase class I enzymes are central regulators of epigenetic silencing through their enzymatic removal of acetyl groups from nuclear proteins, primarily within multi-protein repressor complexes. They are important drug targets across oncology and neurology fields due to their broad impact on gene expression programs. Class I HDACs include HDAC1, HDAC2, HDAC3, and HDAC8, which function as part of large multiprotein complexes such as NuRD, Sin3, CoREST, MiDAC, and SMRT/NCoR. Dysregulation of Class I HDACs has been linked to various diseases, including cancers and neurological disorders like schizophrenia. Inhibitors are under clinical investigation or approved for certain cancers.

Other names
HDAC1HDAC2HDAC3HDAC8
02

Mechanism of action

Inhibition of histone deacetylase activity, leading to increased histone acetylation and altered gene expression.

03

Biological functions

Chromatin condensationTranscriptional repressionEpigenetic regulationGene expression controlRegulation of post-translational modifications
04

Disease associations

CancerNeurological disordersSchizophrenia
05

Safety considerations

Broad effects of pan-HDAC inhibitorsPotential for off-target effectsNeed for selective inhibitors for improved therapeutic window
06

Interacting drugs

Entinostat/MS275

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