Tclin HDAC1 Histone deacetylase 1

Protein Summary

Description

Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Deacetylates SP proteins, SP1 and SP3, and regulates their function. Component of the BRG1-RB1-HDAC1 complex, which negatively regulates the CREST-mediated transcription in resting neurons. Upon calcium stimulation, HDAC1 is released from the complex and CREBBP is recruited, which facilitates transcriptional activation. Deacetylates TSHZ3 and regulates its transcriptional repressor activity. Deacetylates 'Lys-310' in RELA and thereby inhibits the transcriptional activity of NF-kappa-B. Deacetylates NR1D2 and abrogates the effect of KAT5-mediated relieving of NR1D2 transcription repression activity. 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. Involved in CIART-mediated transcriptional repression of the circadian transcriptional activator: CLOCK-ARNTL/BMAL1 heterodimer. Required for the transcriptional repression of circadian target genes, such as PER1, mediated by the large PER complex or CRY1 through histone deacetylation. Histone acetylation and deacetylation, catalyzed by multisubunit complexes, play a key role in the regulation of eukaryotic gene expression. The protein encoded by this gene belongs to the histone deacetylase/acuc/apha family and is a component of the histone deacetylase complex. It also interacts with retinoblastoma tumor-suppressor protein and this complex is a key element in the control of cell proliferation and differentiation. Together with metastasis-associated protein-2, it deacetylates p53 and modulates its effect on cell growth and apoptosis. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• Q13547
• Q92534
• HD1

Gene Name

• HDAC1

Ensembl ID

• ENST00000373548
• ENSP00000362649
• ENSG00000116478

Symbol

• RPD3L1
• HD1
• RPD3
• KDAC1
• GON-10
• RPD3L1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
co-expressed gene	1
hub protein	1
interacting protein	1
molecular function	1
protein complex	1

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1472.86   (req: < 5)

Gene RIFs: 326   (req: <= 3)

Antibodies: 1453   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1472.86   (req: >= 5)

Gene RIFs: 326   (req: > 3)

Antibodies: 1453   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 58

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 3326

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 6

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Related Tools

Target Illumination GWAS Analytics (TIGA)

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GENEVA

GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.

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GlyGen

GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.

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ARCHS4

ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.

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Approved Drugs (6)

Explore Approved Drugs

1 – 6 of 6

vorinostat

HDAC1Tclin Epigenetic

INHIBITOR pKi : 8.89

romidepsin

HDAC1Tclin Epigenetic

INHIBITOR pKi : 5.96

belinostat

HDAC1Tclin Epigenetic

INHIBITOR pKi : 9.07

panobinostat

HDAC1Tclin Epigenetic

INHIBITOR pKi : 9

chidamide

HDAC1Tclin Epigenetic

INHIBITOR pIC50 : 7.02

valproic acid

HDAC1Tclin Epigenetic

pIC50 : 3.4

Active Ligands (3326)

Explore Active Ligands

1 – 10 of 3326

fimepinostat

HDAC1Tclin Epigenetic

pIC50 : 9.44

trichostatin

HDAC1Tclin Epigenetic

pKi : 9.06

CUDC-101

HDAC1Tclin Epigenetic

pIC50 : 8.35

Belinosta

HDAC1Tclin Epigenetic

pKi : 7.58

CHEMBL1830424

HDAC1Tclin Epigenetic

pKi : 7.72

dacinostat

HDAC1Tclin Epigenetic

pKi : 9.22

KA1010

HDAC1Tclin Epigenetic

pIC50 : 6.45

pracinostat

HDAC1Tclin Epigenetic

pKi : 7.55

quisinostat

HDAC1Tclin Epigenetic

pKi : 8.14

scriptaid

HDAC1Tclin Epigenetic

pKi : 8.82

Protein-Protein Interactions (878)

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1 – 10 of 878

• See Interactions on String-DB

DNTTIP1

Tbio

Family:  Enzyme

Novelty:  0.1659073

p_int:  1

Score:  0.948

Data Source:  BioPlex,STRINGDB

SINHCAF

Tdark

Novelty:  0.18692832

p_int:  1

Score:  0.941

Data Source:  BioPlex,STRINGDB

ELMSAN1

Tdark

Novelty:  0.65752788

p_int:  1

Score:  0.719

Data Source:  BioPlex,STRINGDB

ZNF219

Tbio

Family:  TF

Novelty:  0.17515242

p_int:  1

Score:  0.606

Data Source:  BioPlex,STRINGDB

MIER2

Tbio

Novelty:  0.85226416

p_int:  1

Score:  0.458

Data Source:  BioPlex,STRINGDB

GATAD2B

Tbio

Family:  TF

Novelty:  0.056775

p_int:  0.999999999

p_ni:  1e-9

Score:  0.983

Data Source:  BioPlex,STRINGDB

HMG20A

Tbio

Family:  TF

Novelty:  0.11994252

p_int:  0.999999998

p_ni:  2e-9

Score:  0.394

Data Source:  BioPlex,STRINGDB

ZNF217

Tbio

Family:  TF

Novelty:  0.01313576

p_int:  0.999999993

p_ni:  4e-9

p_wrong:  4e-9

Score:  0.965

Data Source:  BioPlex,STRINGDB

HMG20B

Tbio

Family:  TF

Novelty:  0.05983143

p_int:  0.999999986

p_ni:  1.4e-8

Score:  0.981

Data Source:  BioPlex,STRINGDB

RREB1

Tbio

Family:  TF

Novelty:  0.01394277

p_int:  0.999999986

p_ni:  3e-9

p_wrong:  1.1e-8

Score:  0.406

Data Source:  BioPlex,STRINGDB

Pathways (140)

Reactome (76)

KEGG (14)

PathwayCommons (27)

WikiPathways (23)

Cell Cycle (R-HSA-1640170)

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5

1 – 5 of 76

Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Cell Cycle	597 targets	R-HSA-1640170
Reactome	Cell Cycle, Mitotic	495 targets	R-HSA-69278
Reactome	Chromatin modifying enzymes	238 targets	R-HSA-3247509
Reactome	Chromatin organization	238 targets	R-HSA-4839726
Reactome	Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants	58 targets	R-HSA-2894862

Name	Explore in Pharos	Explore in Source
Cell Cycle	597 targets	R-HSA-1640170
Cell Cycle, Mitotic	495 targets	R-HSA-69278
Chromatin modifying enzymes	238 targets	R-HSA-3247509
Chromatin organization	238 targets	R-HSA-4839726
Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants	58 targets	R-HSA-2894862

Gene Ontology Terms (72)

Functions (23)

Components (14)

Processes (35)

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Items per page:

10

1 – 10 of 23

GO Term	Evidence	Assigned by
core promoter sequence-specific DNA binding	Inferred from Direct Assay (IDA)	CAFA
histone deacetylase activity	Inferred from Direct Assay (IDA)	BHF-UCL
protein deacetylase activity	Inferred from Direct Assay (IDA)	UniProtKB
protein N-terminus binding	Inferred from Direct Assay (IDA)	MGI
RNA polymerase II proximal promoter sequence-specific DNA binding	Inferred from Direct Assay (IDA)	UniProtKB
transcription corepressor activity	Inferred from Direct Assay (IDA)	BHF-UCL
transcription regulatory region DNA binding	Inferred from Direct Assay (IDA)	ParkinsonsUK-UCL
activating transcription factor binding	Inferred from Physical Interaction (IPI)	UniProtKB
enzyme binding	Inferred from Physical Interaction (IPI)	UniProtKB
histone deacetylase binding	Inferred from Physical Interaction (IPI)	UniProtKB

GWAS Traits (1)

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5

1 – 1 of 1

GWAS Trait	EFO ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
viral load	EFO_0010125	1	1	1		66

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5

1 – 1 of 1

GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
viral load	EFO_0010125	1		66

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Find similar targets by:

UniProt Keyword Find Similar Targets

No Header	No Header
3D-structure
Acetylation
Biological rhythms
Chromatin regulator
Complete proteome
Hydrolase
Isopeptide bond
Methylation
Nucleus
Phosphoprotein

GWAS Trait Find Similar Targets

No Header	No Header
viral load

MGI Phenotype Find Similar Targets

No Header	No Header
cardiovascular system phenotype
cellular phenotype
craniofacial phenotype
embryo phenotype
endocrine/exocrine gland phenotype
growth/size/body region phenotype
integument phenotype
limbs/digits/tail phenotype
mortality/aging
pigmentation phenotype

Orthologs (14)

1 – 5 of 14

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Macaque	histone deacetylase 1		708441
Mouse	histone deacetylase 1	MGI:108086	433759
Rat	histone deacetylase 1	RGD:1309799	297893
Dog	histone deacetylase 1	VGNC:50625	487309
Horse	histone deacetylase 1	VGNC:50592	100070281

Species	Name	OMA	EggNOG	Inparanoid
Macaque	histone deacetylase 1
Mouse	histone deacetylase 1
Rat	histone deacetylase 1
Dog	histone deacetylase 1
Horse	histone deacetylase 1

Publication Statistics

PubMed Score 1472.86

PubMed score by year

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PubTator Score 1010.44

PubTator score by year

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