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histone deacetylase 1

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Target not currently curated in GtoImmuPdb

Target id: 2658

Nomenclature: histone deacetylase 1

Family: 3.5.1.- Histone deacetylases (HDACs)

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 482 1p35.2-p35.1 HDAC1 histone deacetylase 1
Mouse - 482 4 63.26 cM Hdac1 histone deacetylase 1
Rat - 482 5q36 Hdac1 histone deacetylase 1
Database Links Click here for help
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 3.5.1.98

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
romidepsin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 11.8 pKi 3
pKi 11.8 (Ki 1.5x10-12 M) [3]
apicidin Small molecule or natural product Click here for species-specific activity table Hs Inhibition 10.4 pKi 3
pKi 10.4 (Ki 4x10-11 M) [3]
trichostatin A Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.7 pKi 3
pKi 9.7 (Ki 2x10-10 M) [3]
dacinostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.3 pKi 3
pKi 9.3 (Ki 5.5x10-10 M) [3]
belinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.1 pKi 3
pKi 9.1 (Ki 8.5x10-10 M) [3]
vorinostat Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.9 pKi 3
pKi 8.9 (Ki 1.3x10-9 M) [3]
scriptaid Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.8 pKi 3
pKi 8.8 (Ki 1.5x10-9 M) [3]
givinostat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pKi 3
pKi 8.7 (Ki 2x10-9 M) [3]
mocetinostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pKi 3
pKi 8.1 (Ki 9x10-9 M) [3]
entinostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pKi 3
pKi 7.7 (Ki 2.2x10-8 M) [3]
RGFP109 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.5 pKi 21
pKi 7.5 (Ki 3.2x10-8 M) [21]
tacedinaline Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.3 pKi 3
pKi 7.3 (Ki 5x10-8 M) [3]
panobinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pEC50 10
pEC50 8.5 (EC50 3x10-9 M) [10]
givinostat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pEC50 10
pEC50 7.6 (EC50 2.8x10-8 M) [10]
belinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pEC50 10
pEC50 7.4 (EC50 4.1x10-8 M) [10]
entinostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pEC50 10
pEC50 6.7 (EC50 1.81x10-7 M) [10]
quisinostat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 10.0 pIC50 1
pIC50 10.0 (IC50 1.1x10-10 M) [1]
martinostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.5 pIC50 24
pIC50 9.5 (IC50 3x10-10 M) [24]
fimepinostat Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.8 pIC50 20
pIC50 8.8 (IC50 1.7x10-9 M) [20]
CHR-3996 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.5 pIC50 16
pIC50 8.5 (IC50 3x10-9 M) [16]
CUDC-101 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 5
pIC50 8.4 (IC50 4.5x10-9 M) [5]
abexinostat Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.1 pIC50 4
pIC50 8.1 (IC50 7x10-9 M) [4]
citarinostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.5 pIC50 8
pIC50 7.5 (IC50 3.5x10-8 M) [8]
resminostat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pIC50 14
pIC50 7.4 (IC50 4.25x10-8 M) [14]
pracinostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 pIC50 18
pIC50 7.3 (IC50 4.9x10-8 M) [18]
ricolinostat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 22
pIC50 7.2 (IC50 5.8x10-8 M) [22]
ACY-738 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 9
pIC50 7.0 (IC50 9.4x10-8 M) [9]
BML-281 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.0 pIC50 12
pIC50 7.0 (IC50 1x10-7 M) [12]
suprastat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pIC50 17
pIC50 6.9 (IC50 1.17x10-7 M) [17]
KA1010 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.4 pIC50 6
pIC50 6.4 (IC50 3.56x10-7 M) [6]
tacedinaline Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pIC50 15
pIC50 6.2 (IC50 5.7x10-7 M) [15]
SS-208 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.9 pIC50 23
pIC50 5.9 (IC50 1.39x10-6 M) [23]
nexturastat A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 5.5 pIC50 2
pIC50 5.5 (IC50 3.002x10-6 M) [2]
tubastatin A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 4.9 pIC50 11
pIC50 4.9 (IC50 1.38x10-5 M) [11]
butyric acid Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 4.8 pIC50 7
pIC50 4.8 (IC50 1.6x10-5 M) [7]
valproic acid Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibition 3.4 pIC50 19
pIC50 3.4 (IC50 4x10-4 M) [19]
tucidinostat Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition - - 13
[13]
Immuno Process Associations
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:0045652 regulation of megakaryocyte differentiation TAS
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0045652 regulation of megakaryocyte differentiation TAS
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:2000343 positive regulation of chemokine (C-X-C motif) ligand 2 production ISO
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 3 GO processes
GO:0032732 positive regulation of interleukin-1 production ISO
GO:0032760 positive regulation of tumor necrosis factor production ISO
GO:2000343 positive regulation of chemokine (C-X-C motif) ligand 2 production ISO
General Comments
HDAC1 is a Class I histone deacetylase.

References

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1. Arts J, King P, Mariën A, Floren W, Beliën A, Janssen L, Pilatte I, Roux B, Decrane L, Gilissen R et al.. (2009) JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin. Cancer Res., 15 (22): 6841-51. [PMID:19861438]

2. Bergman JA, Woan K, Perez-Villarroel P, Villagra A, Sotomayor EM, Kozikowski AP. (2012) Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. J. Med. Chem., 55 (22): 9891-9. [PMID:23009203]

3. Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R. (2010) Chemical phylogenetics of histone deacetylases. Nat. Chem. Biol., 6 (3): 238-243. [PMID:20139990]

4. Buggy JJ, Cao ZA, Bass KE, Verner E, Balasubramanian S, Liu L, Schultz BE, Young PR, Dalrymple SA. (2006) CRA-024781: a novel synthetic inhibitor of histone deacetylase enzymes with antitumor activity in vitro and in vivo. Mol. Cancer Ther., 5 (5): 1309-17. [PMID:16731764]

5. Cai X, Zhai HX, Wang J, Forrester J, Qu H, Yin L, Lai CJ, Bao R, Qian C. (2010) Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. J. Med. Chem., 53 (5): 2000-9. [PMID:20143778]

6. Ellis JD, Neil DA, Inston NG, Jenkinson E, Drayson MT, Hampson P, Shuttleworth SJ, Ready AR, Cobbold M. (2016) Inhibition of Histone Deacetylase 6 Reveals a Potent Immunosuppressant Effect in Models of Transplantation. Transplantation, 100 (8): 1667-74. [PMID:27222932]

7. Fass DM, Shah R, Ghosh B, Hennig K, Norton S, Zhao WN, Reis SA, Klein PS, Mazitschek R, Maglathlin RL et al.. (2010) Effect of Inhibiting Histone Deacetylase with Short-Chain Carboxylic Acids and Their Hydroxamic Acid Analogs on Vertebrate Development and Neuronal Chromatin. ACS Med Chem Lett, 2 (1): 39-42. [PMID:21874153]

8. Huang P, Almeciga-Pinto I, Jarpe M, van Duzer JH, Mazitschek R, Yang M, Jones SS, Quayle SN. (2017) Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models. Oncotarget, 8 (2): 2694-2707. [PMID:27926524]

9. Jochems J, Boulden J, Lee BG, Blendy JA, Jarpe M, Mazitschek R, Van Duzer JH, Jones S, Berton O. (2014) Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology, 39 (2): 389-400. [PMID:23954848]

10. Khan N, Jeffers M, Kumar S, Hackett C, Boldog F, Khramtsov N, Qian X, Mills E, Berghs SC, Carey N et al.. (2008) Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. Biochem. J., 409 (2): 581-9. [PMID:17868033]

11. Kozikowski A, Butler KV, Kalin JH. (2014) HDAC inhibitors and therapeutic methods of using same. Patent number: US8748451. Assignee: The Board Of Trustees Of The University Of Illinois. Priority date: 22/07/2009. Publication date: 10/06/2014.

12. Kozikowski AP, Tapadar S, Luchini DN, Kim KH, Billadeau DD. (2008) Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. J. Med. Chem., 51 (15): 4370-3. [PMID:18642892]

13. Liu L, Chen B, Qin S, Li S, He X, Qiu S, Zhao W, Zhao H. (2010) A novel histone deacetylase inhibitor Chidamide induces apoptosis of human colon cancer cells. Biochem. Biophys. Res. Commun., 392 (2): 190-5. [PMID:20060381]

14. Mandl-Weber S, Meinel FG, Jankowsky R, Oduncu F, Schmidmaier R, Baumann P. (2010) The novel inhibitor of histone deacetylase resminostat (RAS2410) inhibits proliferation and induces apoptosis in multiple myeloma (MM) cells. Br. J. Haematol., 149 (4): 518-28. [PMID:20201941]

15. Methot JL, Chakravarty PK, Chenard M, Close J, Cruz JC, Dahlberg WK, Fleming J, Hamblett CL, Hamill JE, Harrington P et al.. (2008) Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2). Bioorg. Med. Chem. Lett., 18 (3): 973-8. [PMID:18182289]

16. Moffat D, Patel S, Day F, Belfield A, Donald A, Rowlands M, Wibawa J, Brotherton D, Stimson L, Clark V et al.. (2010) Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor. J. Med. Chem., 53 (24): 8663-78. [PMID:21080647]

17. Noonepalle S, Shen S, Ptáček J, Tavares MT, Zhang G, Stránský J, Pavlíček J, Ferreira GM, Hadley M, Pelaez G et al.. (2020) Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models. J Med Chem, 63 (18): 10246-10262. [PMID:32815366]

18. Novotny-Diermayr V, Sangthongpitag K, Hu CY, Wu X, Sausgruber N, Yeo P, Greicius G, Pettersson S, Liang AL, Loh YK et al.. (2010) SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer. Mol. Cancer Ther., 9 (3): 642-52. [PMID:20197387]

19. Phiel CJ, Zhang F, Huang EY, Guenther MG, Lazar MA, Klein PS. (2001) Histone deacetylase is a direct target of valproic acid, a potent anticonvulsant, mood stabilizer, and teratogen. J. Biol. Chem., 276 (39): 36734-41. [PMID:11473107]

20. Qian C, Lai CJ, Bao R, Wang DG, Wang J, Xu GX, Atoyan R, Qu H, Yin L, Samson M et al.. (2012) Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling. Clin. Cancer Res., 18 (15): 4104-13. [PMID:22693356]

21. Rai M, Soragni E, Chou CJ, Barnes G, Jones S, Rusche JR, Gottesfeld JM, Pandolfo M. (2010) Two new pimelic diphenylamide HDAC inhibitors induce sustained frataxin upregulation in cells from Friedreich's ataxia patients and in a mouse model. PLoS ONE, 5 (1): e8825. [PMID:20098685]

22. Santo L, Hideshima T, Kung AL, Tseng JC, Tamang D, Yang M, Jarpe M, van Duzer JH, Mazitschek R, Ogier WC et al.. (2012) Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. Blood, 119 (11): 2579-89. [PMID:22262760]

23. Shen S, Hadley M, Ustinova K, Pavlicek J, Knox T, Noonepalle S, Tavares MT, Zimprich CA, Zhang G, Robers MB et al.. (2019) Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models. J. Med. Chem., 62 (18): 8557-8577. [PMID:31414801]

24. Wang C, Schroeder FA, Wey HY, Borra R, Wagner FF, Reis S, Kim SW, Holson EB, Haggarty SJ, Hooker JM. (2014) In vivo imaging of histone deacetylases (HDACs) in the central nervous system and major peripheral organs. J. Med. Chem., 57 (19): 7999-8009. [PMID:25203558]

How to cite this page

3.5.1.- Histone deacetylases (HDACs): histone deacetylase 1. Last modified on 07/09/2020. Accessed on 30/11/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2658.