Histone deacetylase 3
Also known as: HDAC3
Function
Histone deacetylase that catalyzes the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4), and some other non-histone substrates. 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, such as N-Cor repressor complex, which activate the histone deacetylase activity. Participates in the BCL6 transcriptional repressor activity by deacetylating the H3 'Lys-27' (H3K27) on enhancer elements, antagonizing EP300 acetyltransferase activity and repressing proximal gene expression. Acts as a molecular chaperone for shuttling phosphorylated NR2C1 to PML bodies for sumoylation (By similarity). Contributes, together with XBP1 isoform 1, to the activation of NFE2L2-mediated HMOX1 transcription factor gene expression in a PI(3)K/mTORC2/Akt-dependent signaling pathway leading to endothelial cell (EC) survival under disturbed flow/oxidative stress. Regulates both the transcriptional activation and repression phases of the circadian clock in a deacetylase activity-independent manner (By similarity). During the activation phase, promotes the accumulation of ubiquitinated BMAL1 at the E-boxes and during the repression phase, blocks FBXL3-mediated CRY1/2 ubiquitination and promotes the interaction of CRY1 and BMAL1 (By similarity). The NCOR1-HDAC3 complex regulates the circadian expression of the core clock gene BMAL1 and the genes involved in lipid metabolism in the liver (By similarity). Also functions as a deacetylase for non-histone targets, such as KAT5, MEF2D, MAPK14, RARA and STAT3. Serves as a corepressor of RARA, mediating its deacetylation and repression, leading to inhibition of RARE DNA element binding. In association with RARA, plays a role in the repression of microRNA-10a and thereby in the inflammatory response. 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), 2-hydroxyisobutanoyl (2-hydroxyisobutyryl) and isonicotinyl acyl groups from lysine residues, leading to protein decrotonylation, delactylation, de-2-hydroxyisobutyrylation and deisonicotinylation, respectively. Catalyzes decrotonylation of MAPRE1/EB1. Mediates delactylation NBN/NBS1, thereby inhibiting DNA double-strand breaks (DSBs) via homologous recombination (HR).
Classification
- Family (Pfam)
- PF00850 Hist_deacetyl
- InterPro
- HDAC_I/II, HDACs, His_deacetylse_dom, His_deacetylse_dom_sf, Ureohydrolase_dom_sf
- Functional cluster
- Nucleotide & Amino-Acid Biosynthesis Enzymes
Experimental structures · PDB · 1
- 4A69 X-ray 2.06A
A predicted model is available from AlphaFold.
Gene Ontology · 64
- GO:0000785 chromatin
- GO:0005737 cytoplasm
- GO:0005829 cytosol
- GO:0000118 histone deacetylase complex
- GO:0072686 mitotic spindle
- GO:0005654 nucleoplasm
- GO:0005634 nucleus
- GO:0017053 transcription repressor complex
- GO:0003682 chromatin binding
- GO:0031490 chromatin DNA binding
- GO:0030332 cyclin binding
- GO:0140297 DNA-binding transcription factor binding
- GO:0019899 enzyme binding
- GO:0051020 GTPase binding
- GO:0004407 histone deacetylase activity
- GO:0141221 histone deacetylase activity, hydrolytic mechanism
- GO:0042826 histone deacetylase binding
- GO:0160009 histone decrotonylase activity
- GO:0140229 histone isonicotinyllysine deisonicotinylase activity
- GO:0051059 NF-kappaB binding
- GO:0160010 protein de-2-hydroxyisobutyrylase activity
- GO:0160008 protein decrotonylase activity
- GO:0033558 protein lysine deacetylase activity
- GO:0160216 protein lysine delactylase activity
- GO:0003714 transcription corepressor activity
- GO:0001222 transcription corepressor binding
- GO:1990381 ubiquitin-specific protease binding
- GO:0071498 cellular response to fluid shear stress
- GO:0071260 cellular response to mechanical stimulus
- GO:0071374 cellular response to parathyroid hormone stimulus
- GO:0006325 chromatin organization
- GO:0032922 circadian regulation of gene expression
- GO:1903575 cornified envelope assembly
- GO:0140861 DNA repair-dependent chromatin remodeling
- GO:0006351 DNA-templated transcription
- GO:0040029 epigenetic regulation of gene expression
- GO:0000132 establishment of mitotic spindle orientation
- GO:0061436 establishment of skin barrier
- GO:0001701 in utero embryonic development
- GO:0043066 negative regulation of apoptotic process
- GO:0045892 negative regulation of DNA-templated transcription
- GO:0032692 negative regulation of interleukin-1 production
- GO:0046329 negative regulation of JNK cascade
- GO:0046826 negative regulation of protein export from nucleus
- GO:0000122 negative regulation of transcription by RNA polymerase II
- GO:0060633 negative regulation of transcription initiation by RNA polymerase II
- GO:0032720 negative regulation of tumor necrosis factor production
- GO:0120162 positive regulation of cold-induced thermogenesis
- GO:0160020 positive regulation of ferroptosis
- GO:0043525 positive regulation of neuron apoptotic process
- GO:0042307 positive regulation of protein import into nucleus
- GO:0001934 positive regulation of protein phosphorylation
- GO:0031398 positive regulation of protein ubiquitination
- GO:0032008 positive regulation of TOR signaling
- GO:0045944 positive regulation of transcription by RNA polymerase II
- GO:2000676 positive regulation of type B pancreatic cell apoptotic process
- GO:0006476 protein deacetylation
- GO:0060816 random inactivation of X chromosome
- GO:0042752 regulation of circadian rhythm
- GO:0031647 regulation of protein stability
- GO:0071548 response to dexamethasone
- GO:0031667 response to nutrient levels
- GO:0009410 response to xenobiotic stimulus
- GO:0051225 spindle assembly
Drugs targeting this protein · 12
- ABEXINOSTAT inhibitor
- QUISINOSTAT inhibitor
- TACEDINALINE inhibitor
- MOCETINOSTAT inhibitor
- ENTINOSTAT inhibitor
- ROMIDEPSIN inhibitor
- PANOBINOSTAT LACTATE inhibitor
- FIMEPINOSTAT inhibitor
- BELINOSTAT inhibitor
- CUDC-101 inhibitor
- GIVINOSTAT HYDROCHLORIDE inhibitor
- VORINOSTAT inhibitor
Related proteins · sequence + function similarity
- Histone deacetylase 3 1.00
- Histone deacetylase 3 1.00
- Histone deacetylase 3 1.00
- Histone deacetylase 3 1.00
- Histone deacetylase 3 0.99
- Histone deacetylase 3 0.99
- Histone deacetylase 3 0.99
- Histone deacetylase 3 0.98
- Histone deacetylase B 0.95
- Histone deacetylase 9 0.95
- Histone deacetylase clr6 0.93
- Histone deacetylase phd1 0.93
Co-cited proteins · studied together in the literature
- Nuclear receptor corepressor 2 6 shared papers
- Polyamine deacetylase HDAC10 1 shared papers
- F-box-like/WD repeat-containing protein TBL1X 4 shared papers
- Histone deacetylase 1 13 shared papers
- Ubiquitin carboxyl-terminal hydrolase 38 1 shared papers
- NF-kappa-B-activating protein 1 shared papers
- Insulinoma-associated protein 1 2 shared papers
- Coronin-2A 1 shared papers
- Histone deacetylase 7 2 shared papers
- X-box-binding protein 1 1 shared papers
- Immediate early protein IE1 1 shared papers
- Histone acetyltransferase KAT5 4 shared papers
Literature · 47 cited papers
- NBS1 lactylation is required for efficient DNA repair and chemotherapy resistance. Nature · 2024
- Class I histone deacetylases (HDAC1-3) are histone lysine delactylases. Sci. Adv. · 2022
- Dynamic crotonylation of EB1 by TIP60 ensures accurate spindle positioning in mitosis. Nat. Chem. Biol. · 2021
- Isonicotinylation is a histone mark induced by the anti-tuberculosis first-line drug isoniazid. Nat. Commun. · 2021
- USP38 regulates the stemness and chemoresistance of human colorectal cancer via regulation of HDAC3. Oncogenesis · 2020
- Landscape of the regulatory elements for lysine 2-hydroxyisobutyrylation pathway. Cell Res. · 2018
- Class I histone deacetylases are major histone decrotonylases: evidence for critical and broad function of histone crotonylation in transcription. Cell Res. · 2017
- MicroRNA-10a is crucial for endothelial response to different flow patterns via interaction of retinoid acid receptors and histone deacetylases. Proc. Natl. Acad. Sci. U.S.A. · 2017
- Regulation of histone acetyltransferase TIP60 function by histone deacetylase 3. J. Biol. Chem. · 2014
- Unspliced X-box-binding protein 1 (XBP1) protects endothelial cells from oxidative stress through interaction with histone deacetylase 3. J. Biol. Chem. · 2014
- A hybrid mechanism of action for BCL6 in B cells defined by formation of functionally distinct complexes at enhancers and promoters. Cell Rep. · 2013
- Toward a comprehensive characterization of a human cancer cell phosphoproteome. J. Proteome Res. · 2013
- … and 35 more in the literature graph