Protein / target

Histone deacetylase 2

HDAC2Q92769Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
8
Approved medicines
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Histone deacetylase activity, hydrolytic mechanism

Primary system

Nervous system

Strongest disease association

neoplasm

Literature evidence · score 0.57

Therapeutic maturity

Clinically validated target

8 approved medicines against this target

Druggability

Small molecule

Open Targets tractability · Approved Drug

Clinical development

8 approved · 6 in clinical development

30 linked trials

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function

Histone deacetylase that catalyzes the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4) (PubMed:28497810). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events (By similarity). Histone deacetylases act via the formation of large multiprotein complexes (By similarity). Forms transcriptional repressor complexes by associating with MAD, SIN3, YY1 and N-COR (PubMed:12724404). Component of a RCOR/GFI/KDM1A/HDAC complex that suppresses, via histone deacetylase (HDAC) recruitment, a number of genes implicated in multilineage blood cell development (By similarity). Acts as a component of the histone deacetylase NuRD complex which participates in the remodeling of chromatin (PubMed:16428440, PubMed:28977666). Component of the SIN3B complex that represses transcription and counteracts the histone acetyltransferase activity of EP300 through the recognition H3K27ac marks by PHF12 and the activity of the histone deacetylase HDAC2 (PubMed:37137925). Also deacetylates non-histone targets: deacetylates TSHZ3, thereby regulating its transcriptional repressor activity (PubMed:19343227). May be involved in the transcriptional repression of circadian target genes, such as PER1, mediated by CRY1 through histone deacetylation (By similarity). Involved in MTA1-mediated transcriptional corepression of TFF1 and CDKN1A (PubMed:21965678). In addition to protein deacetylase activity, also acts as a protein-lysine deacylase by recognizing other acyl groups: catalyzes removal of (2E)-butenoyl (crotonyl), lactoyl (lactyl) and 2-hydroxyisobutanoyl (2-hydroxyisobutyryl) acyl groups from lysine residues, leading to protein decrotonylation, delactylation and de-2-hydroxyisobutyrylation, respectively (PubMed:28497810, PubMed:29192674, PubMed:35044827)

Subcellular location

NucleusCytoplasm
Domains and Gene Ontology detail (76)

Gene Ontology

  • Cchromatin
  • Cchromosome, telomeric region
  • Ccytoplasm
  • CESC/E(Z) complex
  • Chistone deacetylase complex
  • Cnucleoplasm
  • Cnucleus
  • CNuRD complex
  • Cprotein-containing complex
  • CSin3-type complex
  • Fchromatin binding
  • Fenzyme binding

488 aa · 55 kDa · 2 isoforms

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Transcriptional regulationUniProt · GO · ReactomeImmune signallingGOProteolysisGOMetabolic enzyme activityUniProtApoptosis & cell deathGOHaemostasisReactome
View supporting evidence

Transcriptional regulation

  • ·Histone deacetylase that catalyzes the deacetylation of lysine residues on the N-termina…
  • ·RNA polymerase II-specific DNA-binding transcription factor binding
  • ·transcription coregulator binding
  • ·circadian regulation of gene expression

Immune signalling

  • ·positive regulation of interleukin-1 production

Proteolysis

  • ·positive regulation of proteolysis

Metabolic enzyme activity

  • ·Histone deacetylase that catalyzes the deacetylation of lysine residues on the N-termina…

Apoptosis & cell death

  • ·negative regulation of apoptotic process

Haemostasis

  • ·Factors involved in megakaryocyte development and platelet production
View underlying pathways (25)

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.

DNMT1EZH2SIN3BMTA2HDAC1CHD4CHD3SMARCA4SAP30RBBP4HDAC2

10 strongest partners — larger node and heavier line mean higher confidence

Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.

Drugs targeting this protein

1

Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.

vorinostat
ApprovedInhibitor

Histone deacetylase 2 inhibitor

Appears in clinical studies involving T-cell non-Hodgkin lymphoma, primary cutaneous T-cell non-Hodgkin lymphoma, primary cutaneous T-cell non-Hodgkin lymphoma, neoplasm

Direct interaction with this protein · 1 of 4 recorded protein targets

ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.

Translational evidence

Open Targets 26

Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.

Highest-confidence therapeutic associations

Diseases where a drug acting on this target has already reached clinical development.

primary cutaneous T-cell non-Hodgkin lymphoma0.92

Clinical · overall 0.57

plasma cell myeloma0.92

Clinical · overall 0.56

neoplasm0.89

Clinical · overall 0.57

Duchenne muscular dystrophy0.85

Clinical · overall 0.52

T-cell non-Hodgkin lymphoma0.85

Clinical · overall 0.52

Highest overall evidence

Remaining associations by Open Targets' aggregated evidence score.

neurodegenerative disease0.52

Pathway

peripheral T-cell lymphoma, not otherwise specified0.52

Clinical

mature T-cell and NK-cell non-Hodgkin lymphoma0.51

Clinical

breast cancer0.40

Literature

acute myeloid leukemia0.39

Literature

Show all associations
neoplasm0.57
primary cutaneous T-cell non-Hodgkin lymphoma0.57
plasma cell myeloma0.56
Duchenne muscular dystrophy0.52
neurodegenerative disease0.52
T-cell non-Hodgkin lymphoma0.52
peripheral T-cell lymphoma, not otherwise specified0.52
mature T-cell and NK-cell non-Hodgkin lymphoma0.51
breast cancer0.40
acute myeloid leukemia0.39

Open Targets ranks 1,412 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.

Known drugs · 14 total

QUISINOSTATPhase 2

primary cutaneous T-cell non-Hodgkin lymphoma · ovarian carcinoma · malignant epithelial tumor of ovary

MOCETINOSTATPhase 2

non-small cell lung carcinoma · Hodgkins lymphoma · classic Hodgkin lymphoma

GIVINOSTAT HYDROCHLORIDEApproval

Duchenne muscular dystrophy · Duchenne muscular dystrophy · acquired polycythemia vera

PANOBINOSTATApproval

plasma cell myeloma · neoplasm · type 2 diabetes mellitus

PANOBINOSTAT LACTATEApproval

plasma cell myeloma

TACEDINALINEPhase 3

non-small cell lung carcinoma · exocrine pancreatic carcinoma

BELINOSTATApproval

T-cell non-Hodgkin lymphoma · peripheral T-cell lymphoma, not otherwise specified · neoplasm

ROMIDEPSINApproval

T-cell non-Hodgkin lymphoma · peripheral T-cell lymphoma, not otherwise specified · primary cutaneous T-cell non-Hodgkin lymphoma

GIVINOSTATApproval

Duchenne muscular dystrophy · Duchenne muscular dystrophy · acquired polycythemia vera

FIMEPINOSTATPhase 2

diffuse large B-cell lymphoma · thyroid cancer · poorly differentiated thyroid gland carcinoma

Tractability

SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Med-Quality PocketSM · Druggable FamilyPR · LiteraturePR · UniProt UbiquitinationPR · Database UbiquitinationPR · Half-life DataPR · Small Molecule BinderOC · Approved Drug

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.

Show remaining trials (24)

TERMINATED · via vorinostat · NCT01483690

COMPLETED · via vorinostat · NCT03259503

ClinicalTrials.gov via the drug-target graph.

Forefront confidence

Synthesis

Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.

neoplasmModerately supported
0.72
agreement 0.560.87
Clinical82%Literature18%

Open Targets aggregate 0.57 · 2 independent evidence families

primary cutaneous T-cell non-Hodgkin lymphomaModerately supported
0.70
agreement 0.550.86
Clinical95%Literature5%

Open Targets aggregate 0.57 · 2 independent evidence families

plasma cell myelomaModerately supported
0.69
agreement 0.540.85
Clinical98%Literature2%

Open Targets aggregate 0.56 · 2 independent evidence families

Duchenne muscular dystrophyModerately supported
0.65
agreement 0.500.81
Clinical95%Literature5%

Open Targets aggregate 0.52 · 2 independent evidence families

T-cell non-Hodgkin lymphomaModerately supported
0.64
agreement 0.480.79
Clinical99%Literature1%

Open Targets aggregate 0.52 · 2 independent evidence families

The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.

What's happening now

14

Recent activity around this target, drawn from one canonical event stream. Every item is reached through a drug that targets this protein, so each event is news about that drug rather than about the protein directly.

  1. New publication2024-05-01
    Ketogenic Diet Alters the Epigenetic and Immune Landscape of Prostate Cancer to Overcome Resistance to Immune Checkpoint Blockade Therapy.

    Cancer research · 2024 · 47 citations · Europe PMC · via vorinostat

  2. New publication2023-08-24
    Suberoylanilide Hydroxamic Acid (SAHA) Is a Driver Molecule of Neuroplasticity: Implication for Neurological Diseases.

    Biomolecules · 2023 · 9 citations · Europe PMC · via vorinostat

  3. New publication2015-06-20
    Phase I study of the mTOR inhibitor ridaforolimus and the HDAC inhibitor vorinostat in advanced renal cell carcinoma and other solid tumors.

    Investigational new drugs · 2015 · 43 citations · Europe PMC · via vorinostat

  4. New publication2015-03-20
    Vorinostat in patients with advanced malignant pleural mesothelioma who have progressed on previous chemotherapy (VANTAGE-014): a phase 3, double-blind, randomised, placebo-controlled trial.

    The Lancet. Oncology · 2015 · 151 citations · Europe PMC · via vorinostat

  5. New publication2014-11-20
    A phase 1 study of vorinostat maintenance after autologous transplant in high-risk lymphoma.

    Leukemia & lymphoma · 2015 · 6 citations · Europe PMC · via vorinostat

  6. New publication2014-03-12
    A multicentre phase II study of vorinostat in patients with relapsed or refractory indolent B-cell non-Hodgkin lymphoma and mantle cell lymphoma.

    British journal of haematology · 2014 · 89 citations · Europe PMC · via vorinostat

  7. New publication2014-03-11
    HIV-1 expression within resting CD4+ T cells after multiple doses of vorinostat.

    The Journal of infectious diseases · 2014 · 203 citations · Europe PMC · via vorinostat

  8. New publication2014-01-25
    Phase II trial of vorinostat in advanced melanoma.

    Investigational new drugs · 2014 · 46 citations · Europe PMC · via vorinostat

  9. New publication2013-11-30
    Vorinostat plus tacrolimus and mycophenolate to prevent graft-versus-host disease after related-donor reduced-intensity conditioning allogeneic haemopoietic stem-cell transplantation: a phase 1/2 trial.

    The Lancet. Oncology · 2014 · 102 citations · Europe PMC · via vorinostat

  10. New publication2012-07-25
    Administration of vorinostat disrupts HIV-1 latency in patients on antiretroviral therapy.

    Nature · 2012 · 984 citations · Europe PMC · via vorinostat

  11. New publication2012-04-16
    Phase I and pharmacokinetic study of the oral histone deacetylase inhibitor vorinostat in Japanese patients with relapsed or refractory cutaneous T-cell lymphoma.

    The Journal of dermatology · 2012 · 17 citations · Europe PMC · via vorinostat

  12. New publication2012-01-11
    Evaluation of safety, pharmacokinetics, and efficacy of vorinostat, a histone deacetylase inhibitor, in the treatment of gastrointestinal (GI) cancer in a phase I clinical trial.

    International journal of clinical oncology · 2013 · 28 citations · Europe PMC · via vorinostat

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.