histone deacetylase 7

Target id: 2661

Nomenclature: histone deacetylase 7

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 7 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 991 12q13.1 HDAC7 histone deacetylase 7
Mouse - 953 15 F2 Hdac7 histone deacetylase 7
Rat - - 7q36 Hdac7 histone deacetylase 7
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
belinostat Hs Inhibition 7.1 pKi 2
pKi 7.1 (Ki 7.5x10-8 M) [2]
trichostatin A Hs Inhibition 6.7 pKi 2
pKi 6.7 (Ki 1.95x10-7 M) [2]
givinostat Hs Inhibition 6.6 pKi 2
pKi 6.6 (Ki 2.4x10-7 M) [2]
romidepsin Hs Inhibition 5.9 pKi 2
pKi 5.9 (Ki 1.25x10-6 M) [2]
scriptaid Hs Inhibition 5.7 pKi 2
pKi 5.7 (Ki 2.25x10-6 M) [2]
dacinostat Hs Inhibition 5.0 pKi 2
pKi 5.0 (Ki 9.5x10-6 M) [2]
panobinostat Hs Inhibition 7.8 pEC50 6
pEC50 7.8 (EC50 1.4x10-8 M) [6]
belinostat Hs Inhibition 7.2 pEC50 6
pEC50 7.2 (EC50 6.7x10-8 M) [6]
givinostat Hs Inhibition 6.8 pEC50 6
pEC50 6.8 (EC50 1.63x10-7 M) [6]
TMP269 Hs Inhibition 7.4 pIC50 7
pIC50 7.4 (IC50 4.3x10-8 M) [7]
quisinostat Hs Inhibition 6.9 pIC50 1
pIC50 6.9 (IC50 1.19x10-7 M) [1]
CUDC-101 Hs Inhibition 6.4 pIC50 3
pIC50 6.4 (IC50 3.73x10-7 M) [3]
KA1010 Hs Inhibition 6.0 pIC50 5
pIC50 6.0 (IC50 9.86x10-7 M) [5]
General Comments
HDAC7 is a Class II histone deacetylase. This histone deacetylase can associate with at least 12 different proteins, including components of the NuRD and Sin3A repression complexes [4].

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. Downes M, Ordentlich P, Kao HY, Alvarez JG, Evans RM. (2000) Identification of a nuclear domain with deacetylase activity. Proc. Natl. Acad. Sci. U.S.A.97 (19): 10330-5. [PMID:10984530]

5. 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. Transplantation100 (8): 1667-74. [PMID:27222932]

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]

How to cite this page

3.5.1.- Histone deacetylases (HDACs): histone deacetylase 7. Last modified on 25/09/2017. Accessed on 12/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2661.