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Protein / target

Histone deacetylase 1

Encoded byHDAC1Q13547Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
8
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

RNA polymerase II core promoter sequence-specific DNA binding

Strongest disease association

Neoplasms

Via encoding gene HDAC1 · Literature evidence · score 0.57

Therapeutic position

Established drug target

Small molecules

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 overview

Histone deacetylase that catalyzes the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4).

View complete UniProt function annotation

Histone deacetylase that catalyzes the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4) (PubMed:16762839, PubMed:17704056, PubMed:28497810). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events (PubMed:16762839, PubMed:17704056). Histone deacetylases act via the formation of large multiprotein complexes (PubMed:16762839, PubMed:17704056). Acts as a component of the histone deacetylase NuRD complex which participates in the remodeling of chromatin (PubMed:16428440, PubMed:28977666). As part of the SIN3B complex is recruited downstream of the constitutively active genes transcriptional start sites through interaction with histones and mitigates histone acetylation and RNA polymerase II progression within transcribed regions contributing to the regulation of transcription (PubMed:21041482). Also functions as a deacetylase for non-histone targets, such as NR1D2, RELA, SP1, SP3, STAT3, ZNF76 and TSHZ3 (PubMed:12837748, PubMed:16285960, PubMed:16337145, PubMed:16478997, PubMed:17996965, PubMed:19343227). Deacetylates SP proteins, SP1 and SP3, and regulates their function (PubMed:12837748, PubMed:16478997). Component of the BRG1-RB1-HDAC1 complex, which negatively regulates the CREST-mediated transcription in resting neurons (PubMed:19081374). Upon calcium stimulation, HDAC1 is released from the complex and CREBBP is recruited, which facilitates transcriptional activation (PubMed:19081374). Deacetylates TSHZ3 and regulates its transcriptional repressor activity (PubMed:19343227). Deacetylates 'Lys-310' in RELA and thereby inhibits the transcriptional activity of NF-kappa-B (PubMed:17000776). Deacetylates NR1D2 and abrogates the effect of KAT5-mediated relieving of NR1D2 transcription repression activity (PubMed:17996965). 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). Involved in CIART-mediated transcriptional repression of the circadian transcriptional activator: CLOCK-BMAL1 heterodimer (By similarity). Required for the transcriptional repression of circadian target genes, such as PER1, mediated by the large PER complex or CRY1 through histone deacetylation (By similarity). In addition to protein deacetylase activity, also has protein-lysine deacylase activity: acts as a protein decrotonylase and delactylase by mediating decrotonylation ((2E)-butenoyl) and delactylation (lactoyl) of histones, respectively (PubMed:28497810, PubMed:35044827)

Subcellular location

Nucleus
Domains and Gene Ontology detail (68)

Gene Ontology

  • Cchromatin
  • Ccytoplasm
  • Ccytosol
  • Cheterochromatin
  • Chistone deacetylase complex
  • Cneuronal cell body
  • Cnucleoplasm
  • Cnucleus
  • CNuRD complex
  • Cprotein-containing complex
  • Cribonucleoprotein complex
  • CSin3-type complex

482 aa · 55 kDa

Biological roles

Reactome v97

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

Cell proliferation & survivalGOCell migrationGOTranscriptional regulationUniProt · GO · Reactome
View supporting evidence

Cell proliferation & survival

  • ·positive regulation of cell population proliferation

Cell migration

  • ·negative regulation of cell migration

Transcriptional regulation

  • ·Histone deacetylase that catalyzes the deacetylation of lysine residues on the N-termina…
  • ·transcription repressor complex
  • ·DNA-binding transcription factor binding
  • ·RNA polymerase II cis-regulatory region sequence-specific DNA binding
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.

SAP30RBBP7RBBP4SIN3AMBD2CHD4CHD3MECP2EHMT2MTA2HDAC1

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.

Approved medicines with mapped indications

1 medicine · 3 areas

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Lymphoma, T-Cell1 medicine
Lymphoma, T-Cell, Cutaneous1 medicine
Broader indication categories (1)
Neoplasms1 medicine

Broad umbrella indications (e.g. “Neoplasms”). Shown here because every medicine also appears under a more specific disease above — kept for completeness, de-emphasised for clarity.

8 medicines meet Open Targets' target-level approved-medicine definition; the 1 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

1

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

vorinostat
ApprovedInhibitor

Histone deacetylase 1 inhibitor

Indicated for Lymphoma, T-Cell, Lymphoma, T-Cell, Cutaneous, Neoplasms

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

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

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene HDAC1

Gene-level evidence surfaced through the gene HDAC1that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Neoplasms
0.80Well supported

Clinical evidence dominant · Open Targets 0.57

Lymphoma, T-Cell, Cutaneous
0.70Moderately supported

Clinical evidence dominant · Open Targets 0.57

Multiple Myeloma
0.70Moderately supported

Clinical evidence dominant · Open Targets 0.57

Lymphoma, T-Cell
0.65Moderately supported

Clinical evidence dominant · Open Targets 0.52

peripheral T-cell lymphoma, not otherwise specified
0.64Moderately supported

Clinical evidence dominant · Open Targets 0.52

View evidence synthesis (5)
NeoplasmsWell supported
0.80
agreement 0.680.93
Clinical60%Pathway27%Literature13%

Open Targets aggregate 0.57 · 3 independent evidence families

Lymphoma, T-Cell, CutaneousModerately supported
0.70
agreement 0.550.86
Clinical95%Literature5%

Open Targets aggregate 0.57 · 2 independent evidence families

Multiple MyelomaModerately supported
0.70
agreement 0.570.84
Clinical93%Literature6%RNA expression1%

Open Targets aggregate 0.57 · 3 independent evidence families

Lymphoma, T-CellModerately supported
0.65
agreement 0.490.80
Clinical97%Literature4%

Open Targets aggregate 0.52 · 2 independent evidence families

peripheral T-cell lymphoma, not otherwise specifiedModerately supported
0.64
agreement 0.490.80
Clinical98%Literature2%

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 per-type scores above show the calculation.

Show all associations
Neoplasms0.57
Lymphoma, T-Cell, Cutaneous0.57
Multiple Myeloma0.57
Lymphoma, T-Cell0.52
peripheral T-cell lymphoma, not otherwise specified0.52
mature T-cell and NK-cell non-Hodgkin's lymphoma0.51
Leukemia, Myeloid, Acute0.40
Breast Neoplasms0.39

Drug development

14 compounds recorded · 8 approved · 6 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 1 drug that targets this protein in Forefront's canonical graph (1 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (10)
BELINOSTATApproval
FIMEPINOSTATPhase 2
MOCETINOSTATPhase 2
ABEXINOSTATPhase 3
TACEDINALINEPhase 3
GIVINOSTAT HYDROCHLORIDEApproval
ENTINOSTATApproval
QUISINOSTATPhase 2
PANOBINOSTATApproval
VORINOSTATApproval

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesStrong

Approved Drug and Structure with Ligand support this modality.

Protein degradersEmerging

Feasibility evidence (literature and uniprot ubiquitination) — no clinical-stage drug of this modality recorded.

Other modalitiesStrong

Approved Drug support this modality.

View underlying tractability evidence (10)
SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyPR · LiteraturePR · UniProt UbiquitinationPR · Database UbiquitinationPR · Half-life DataPR · Small Molecule BinderOC · Approved Drug

Raw Open Targets tractability assessment buckets, by modality.

Safety-related annotations

regulation of transcription factor activityToxCastNeural tube defectsAOP-WikiNeural tube defectsAOP-WikiFacial cartilage structures are reduced in size and morphologically distortedAOP-WikiTesticular atrophyAOP-Wiki

Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.

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. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

View all trials (26)

RECRUITING · via vorinostat · NCT05848687

ACTIVE_NOT_RECRUITING · via vorinostat · NCT02553460

ACTIVE_NOT_RECRUITING · via vorinostat · NCT01587352

ClinicalTrials.gov via the drug-target graph.

What's happening now

12

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for a drug that targets this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

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

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

  8. 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

  9. 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

  10. 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

  11. New publication2009-12-01
    Evaluation of the long-term tolerability and clinical benefit of vorinostat in patients with advanced cutaneous T-cell lymphoma.

    Clinical lymphoma & myeloma · 2009 · 62 citations · Europe PMC · via vorinostat

  12. New publication2009-11-03
    A single supratherapeutic dose of vorinostat does not prolong the QTc interval in patients with advanced cancer.

    Clinical cancer research : an official journal of the American Association for Cancer Research · 2009 · 32 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.