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histone deacetylase 7

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Target id: 2661

Nomenclature: histone deacetylase 7

Family: 3.5.1.- Histone deacetylases (HDACs)

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 952 12q13.11 HDAC7 histone deacetylase 7
Mouse - 938 15 F1 Hdac7 histone deacetylase 7
Rat - 238 7q36 Hdac7 histone deacetylase 7
Database Links Click here for help
Alphafold Q8WUI4 (Hs), Q8C2B3 (Mm), Q99P96 (Rn)
BRENDA 3.5.1.98
CATH/Gene3D 3.40.800.20
ChEMBL Target CHEMBL2716 (Hs)
Ensembl Gene ENSG00000061273 (Hs), ENSMUSG00000022475 (Mm), ENSRNOG00000055597 (Rn)
Entrez Gene 51564 (Hs), 56233 (Mm), 84582 (Rn)
Human Protein Atlas ENSG00000061273 (Hs)
KEGG Enzyme 3.5.1.98
KEGG Gene hsa:51564 (Hs), mmu:56233 (Mm), rno:84582 (Rn)
OMIM 606542 (Hs)
Pharos Q8WUI4 (Hs)
RefSeq Nucleotide NM_015401 (Hs), NM_001204275 (Mm)
RefSeq Protein NP_056216 (Hs), NP_001191204 (Mm)
UniProtKB Q8WUI4 (Hs), Q8C2B3 (Mm), Q99P96 (Rn)
Wikipedia HDAC7 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.5.1.98

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
belinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pKi 2
⤷ pKi 7.1 (Ki 7.5x10-8 M) [2]
trichostatin A Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pKi 2
⤷ pKi 6.7 (Ki 1.95x10-7 M) [2]
givinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pKi 2
⤷ pKi 6.6 (Ki 2.4x10-7 M) [2]
romidepsin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 5.9 pKi 2
⤷ pKi 5.9 (Ki 1.25x10-6 M) [2]
scriptaid Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.7 pKi 2
⤷ pKi 5.7 (Ki 2.25x10-6 M) [2]
dacinostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.0 pKi 2
⤷ pKi 5.0 (Ki 9.5x10-6 M) [2]
panobinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Guide to Malaria Pharmacology Ligand Hs Inhibition 7.8 pEC50 6
⤷ pEC50 7.8 (EC50 1.4x10-8 M) [6]
belinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pEC50 6
⤷ pEC50 7.2 (EC50 6.7x10-8 M) [6]
givinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.8 pEC50 6
⤷ pEC50 6.8 (EC50 1.63x10-7 M) [6]
TMP269 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pIC50 7
⤷ pIC50 7.4 (IC50 4.3x10-8 M) [7]
quisinostat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Guide to Malaria Pharmacology Ligand Hs Inhibition 6.9 pIC50 1
⤷ pIC50 6.9 (IC50 1.19x10-7 M) [1]
CUDC-101 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 3
⤷ pIC50 6.4 (IC50 3.73x10-7 M) [3]
KA1010 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.0 pIC50 5
⤷ pIC50 6.0 (IC50 9.86x10-7 M) [5]
SS-208 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.1 pIC50 8
⤷ pIC50 5.1 (IC50 8.34x10-6 M) [8]
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
Immuno Process:  B cell (activation)
Immuno Process:  Cellular signalling
Immuno Process:  Immune system development
Immuno Process:  Inflammation
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 USA, 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. 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. 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 7. Last modified on 13/09/2019. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2661.