histone deacetylase 1

Target id: 2658

Nomenclature: histone deacetylase 1

Family: 3.5.1.- Histone deacetylases (HDACs)

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for histone deacetylase 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 482 1p34 HDAC1 histone deacetylase 1
Mouse - 482 4 D2.2 Hdac1 histone deacetylase 1
Rat - 482 5q36 Hdac1 histone deacetylase 1
Database Links
BRENDA
CATH/Gene3D
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.5.1.98

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
romidepsin Hs Inhibition 11.8 pKi 3
pKi 11.8 (Ki 1.5x10-12 M) [3]
apicidin Hs Inhibition 10.4 pKi 3
pKi 10.4 (Ki 4x10-11 M) [3]
trichostatin A Hs Inhibition 9.7 pKi 3
pKi 9.7 (Ki 2x10-10 M) [3]
dacinostat Hs Inhibition 9.3 pKi 3
pKi 9.3 (Ki 5.5x10-10 M) [3]
belinostat Hs Inhibition 9.1 pKi 3
pKi 9.1 (Ki 8.5x10-10 M) [3]
vorinostat Hs Inhibition 8.9 pKi 3
pKi 8.9 (Ki 1.3x10-9 M) [3]
scriptaid Hs Inhibition 8.8 pKi 3
pKi 8.8 (Ki 1.5x10-9 M) [3]
givinostat Hs Inhibition 8.7 pKi 3
pKi 8.7 (Ki 2x10-9 M) [3]
mocetinostat Hs Inhibition 8.1 pKi 3
pKi 8.1 (Ki 9x10-9 M) [3]
entinostat Hs Inhibition 7.7 pKi 3
pKi 7.7 (Ki 2.2x10-8 M) [3]
RGFP109 Hs Inhibition 7.5 pKi 16
pKi 7.5 (Ki 3.2x10-8 M) [16]
tacedinaline Hs Inhibition 7.3 pKi 3
pKi 7.3 (Ki 5x10-8 M) [3]
panobinostat Hs Inhibition 8.5 pEC50 8
pEC50 8.5 (EC50 3x10-9 M) [8]
givinostat Hs Inhibition 7.6 pEC50 8
pEC50 7.6 (EC50 2.8x10-8 M) [8]
belinostat Hs Inhibition 7.4 pEC50 8
pEC50 7.4 (EC50 4.1x10-8 M) [8]
entinostat Hs Inhibition 6.7 pEC50 8
pEC50 6.7 (EC50 1.81x10-7 M) [8]
quisinostat Hs Inhibition 10.0 pIC50 1
pIC50 10.0 (IC50 1.1x10-10 M) [1]
CUDC-907 Hs Inhibition 8.8 pIC50 15
pIC50 8.8 (IC50 1.7x10-9 M) [15]
CHR-3996 Hs Inhibition 8.5 pIC50 12
pIC50 8.5 (IC50 3x10-9 M) [12]
CUDC-101 Hs Inhibition 8.4 pIC50 5
pIC50 8.4 (IC50 4.5x10-9 M) [5]
abexinostat Hs Inhibition 8.1 pIC50 4
pIC50 8.1 (IC50 7x10-9 M) [4]
citarinostat Hs Inhibition 7.5 pIC50 7
pIC50 7.5 (IC50 3.5x10-8 M) [7]
resminostat Hs Inhibition 7.4 pIC50 10
pIC50 7.4 (IC50 4.25x10-8 M) [10]
pracinostat Hs Inhibition 7.3 pIC50 13
pIC50 7.3 (IC50 4.9x10-8 M) [13]
ricolinostat Hs Inhibition 7.2 pIC50 17
pIC50 7.2 (IC50 5.8x10-8 M) [17]
valproic acid Hs Inhibition 6.4 pIC50 14
pIC50 6.4 (IC50 4x10-7 M) [14]
tacedinaline Hs Inhibition 6.2 pIC50 11
pIC50 6.2 (IC50 5.7x10-7 M) [11]
nexturastat A Hs Inhibition 5.5 pIC50 2
pIC50 5.5 (IC50 3.002x10-6 M) [2]
butyric acid Hs Inhibition 4.8 pIC50 6
pIC50 4.8 (IC50 1.6x10-5 M) [6]
tucidinostat Hs Inhibition - - 9
[9]
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. 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 Lett2 (1): 39-42. [PMID:21874153]

7. Huang P, Almeciga-Pinto I, Jarpe M, van Duzer JH, Mazitschek R, Yang M, Jones SS, Quayle SN. (2016) Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models. Oncotarget,  [Epub ahead of print]. [PMID:27926524]

8. 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]

9. 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]

10. 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]

11. 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]

12. 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]

13. 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]

14. 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]

15. 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]

16. 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 ONE5 (1): e8825. [PMID:20098685]

17. 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. Blood119 (11): 2579-89. [PMID:22262760]

How to cite this page

3.5.1.- Histone deacetylases (HDACs): histone deacetylase 1. Last modified on 31/03/2017. Accessed on 19/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2658.