histone deacetylase 5

Target id: 2660

Nomenclature: histone deacetylase 5

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 5 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1122 17q21 HDAC5 histone deacetylase 5
Mouse - 1115 11 D Hdac5 histone deacetylase 5
Rat - 1113 10q32.1 Hdac5 histone deacetylase 5
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 6.8 pKi 2
pKi 6.8 (Ki 1.75x10-7 M) [2]
trichostatin A Hs Inhibition 6.6 pKi 2
pKi 6.6 (Ki 2.6x10-7 M) [2]
dacinostat Hs Inhibition 6.4 pKi 2
pKi 6.4 (Ki 4.2x10-7 M) [2]
romidepsin Hs Inhibition 6.3 pKi 2
pKi 6.3 (Ki 5.5x10-7 M) [2]
givinostat Hs Inhibition 6.2 pKi 2
pKi 6.2 (Ki 6x10-7 M) [2]
scriptaid Hs Inhibition 6.0 pKi 2
pKi 6.0 (Ki 1x10-6 M) [2]
vorinostat Hs Inhibition 5.4 pKi 2
pKi 5.4 (Ki 3.6x10-6 M) [2]
quisinostat Hs Inhibition 8.4 pIC50 1
pIC50 8.4 (IC50 3.69x10-9 M) [1]
CUDC-101 Hs Inhibition 7.9 pIC50 3
pIC50 7.9 (IC50 1.14x10-8 M) [3]
pracinostat Hs Inhibition 7.3 pIC50 8
pIC50 7.3 (IC50 4.7x10-8 M) [8]
TMP269 Hs Inhibition 7.0 pIC50 6
pIC50 7.0 (IC50 9.7x10-8 M) [6]
CHR-3996 Hs Inhibition 6.7 pIC50 7
pIC50 6.7 (IC50 2x10-7 M) [7]
KA1010 Hs Inhibition 6.0 pIC50 5
pIC50 6.0 (IC50 1.093x10-6 M) [5]
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Hdac5+|Hdac5tm1Eno|Pkd2tm2Som Hdac5tm1Eno/Hdac5+,Pkd2tm2Som/Pkd2tm2Som
involves: 129/Sv * 129S2/SvPas * C57BL/6 * SJL
MGI:1099818  MGI:1333784  MP:0003675 kidney cysts PMID: 20181743 
Hdac5tm1Eno|Pkd2tm2Som Hdac5tm1Eno/Hdac5tm1Eno,Pkd2tm2Som/Pkd2tm2Som
involves: 129/Sv * 129S2/SvPas * C57BL/6 * SJL
MGI:1099818  MGI:1333784  MP:0006208 lethality throughout fetal growth and development PMID: 20181743 
General Comments
HDAC5 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. 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]

7. 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]

8. 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]

How to cite this page

3.5.1.- Histone deacetylases (HDACs): histone deacetylase 5. Last modified on 25/09/2017. Accessed on 13/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2660.