histone deacetylase 5 | 3.5.1.- Histone deacetylases (HDACs) | IUPHAR/BPS Guide to PHARMACOLOGY

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histone deacetylase 5

Target not currently curated in GtoImmuPdb

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

Contents:

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 3.5.1.98
CATH/Gene3D 3.40.800.20
ChEMBL Target CHEMBL2563 (Hs), CHEMBL2768 (Mm)
Ensembl Gene ENSG00000108840 (Hs), ENSMUSG00000008855 (Mm), ENSRNOG00000020905 (Rn)
Entrez Gene 10014 (Hs), 15184 (Mm), 84580 (Rn)
Human Protein Atlas ENSG00000108840 (Hs)
KEGG Enzyme 3.5.1.98
KEGG Gene hsa:10014 (Hs), mmu:15184 (Mm), rno:84580 (Rn)
OMIM 605315 (Hs)
RefSeq Nucleotide NM_005474 (Hs), NM_001077696 (Mm), NM_053450 (Rn)
RefSeq Protein NP_005465 (Hs), NP_001071164 (Mm), NP_445902 (Rn)
UniProtKB Q9UQL6 (Hs), Q9Z2V6 (Mm)
Wikipedia HDAC5 (Hs)
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 Value Parameter 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]
SS-208 Hs Inhibition 5.2 pIC50 9
⤷ pIC50 5.2 (IC50 6.91x10-6 M) [9]
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. Transplantation, 100 (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]

9. 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]

How to cite this page

3.5.1.- Histone deacetylases (HDACs): histone deacetylase 5. Last modified on 13/09/2019. Accessed on 24/01/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2660.