histone deacetylase 4

Target id: 2659

Nomenclature: histone deacetylase 4

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 4 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1084 2q37.3 HDAC4 histone deacetylase 4 4
Mouse - 1076 1 D Hdac4 histone deacetylase 4
Rat - 1077 9q36 Hdac4 histone deacetylase 4
Database Links
BRENDA
CATH/Gene3D
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 7.7 pKi 2
pKi 7.7 (Ki 2.05x10-8 M) [2]
belinostat Hs Inhibition 6.4 pKi 2
pKi 6.4 (Ki 3.8x10-7 M) [2]
givinostat Hs Inhibition 6.0 pKi 2
pKi 6.0 (Ki 1.05x10-6 M) [2]
trichostatin A Hs Inhibition 5.8 pKi 2
pKi 5.8 (Ki 1.4x10-6 M) [2]
dacinostat Hs Inhibition 5.7 pKi 2
pKi 5.7 (Ki 2.25x10-6 M) [2]
scriptaid Hs Inhibition 5.1 pKi 2
pKi 5.1 (Ki 7.5x10-6 M) [2]
panobinostat Hs Inhibition 7.9 pEC50 6
pEC50 7.9 (EC50 1.2x10-8 M) [6]
givinostat Hs Inhibition 7.3 pEC50 6
pEC50 7.3 (EC50 5.2x10-8 M) [6]
belinostat Hs Inhibition 6.9 pEC50 6
pEC50 6.9 (EC50 1.15x10-7 M) [6]
quisinostat Hs Inhibition 9.2 pIC50 1
pIC50 9.2 (IC50 6.4x10-10 M) [1]
CUDC-101 Hs Inhibition 7.9 pIC50 3
pIC50 7.9 (IC50 1.32x10-8 M) [3]
TMP269 Hs Inhibition 6.8 pIC50 7
pIC50 6.8 (IC50 1.57x10-7 M) [7]
santacruzamate A Hs Inhibition <6.0 pIC50 8
pIC50 <6.0 (IC50 >1x10-6 M) [8]
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
tasquinimod Hs Inhibition 7.5 – 8.0 pKd 5
pKd 7.5 – 8.0 (Kd 3x10-8 – 1x10-8 M) [5]
Clinically-Relevant Mutations and Pathophysiology
Disease:  Brachydactyly-mental retardation syndrome; BDMR
Synonyms: 2q37 microdeletion syndrome [Orphanet: ORPHA1001]
OMIM: 600430
Orphanet: ORPHA1001
General Comments
HDAC4 is a Class II 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. 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]

3. 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]

4. Grozinger CM, Hassig CA, Schreiber SL. (1999) Three proteins define a class of human histone deacetylases related to yeast Hda1p. Proc. Natl. Acad. Sci. U.S.A.96 (9): 4868-73. [PMID:10220385]

5. Isaacs JT, Antony L, Dalrymple SL, Brennen WN, Gerber S, Hammers H, Wissing M, Kachhap S, Luo J, Xing L et al.. (2013) Tasquinimod Is an Allosteric Modulator of HDAC4 survival signaling within the compromised cancer microenvironment. Cancer Res.73 (4): 1386-99. [PMID:23149916]

6. 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]

7. Lobera M, Madauss KP, Pohlhaus DT, Wright QG, Trocha M, Schmidt DR, Baloglu E, Trump RP, Head MS, Hofmann GA et al.. (2013) Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. Nat. Chem. Biol.9 (5): 319-25. [PMID:23524983]

8. Pavlik CM, Wong CY, Ononye S, Lopez DD, Engene N, McPhail KL, Gerwick WH, Balunas MJ. (2013) Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp. J. Nat. Prod.76 (11): 2026-33. [PMID:24164245]

How to cite this page

3.5.1.- Histone deacetylases (HDACs): histone deacetylase 4. Last modified on 27/10/2015. Accessed on 20/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2659.