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histone deacetylase 11

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Target not currently curated in GtoImmuPdb

Target id: 2615

Nomenclature: histone deacetylase 11

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 - 347 3p25.1 HDAC11 histone deacetylase 11
Mouse - 347 6 D1 Hdac11 histone deacetylase 11
Rat - - 4q34 Hdac11 histone deacetylase 11
Database Links Click here for help
Alphafold Q96DB2 (Hs), Q91WA3 (Mm)
BRENDA 3.5.1.98
CATH/Gene3D 3.40.800.20
ChEMBL Target CHEMBL3310 (Hs)
Ensembl Gene ENSG00000163517 (Hs), ENSMUSG00000034245 (Mm), ENSRNOG00000006824 (Rn)
Entrez Gene 79885 (Hs), 232232 (Mm), 297453 (Rn)
Human Protein Atlas ENSG00000163517 (Hs)
KEGG Enzyme 3.5.1.98
KEGG Gene hsa:79885 (Hs), mmu:232232 (Mm), rno:297453 (Rn)
OMIM 607226 (Hs)
Pharos Q96DB2 (Hs)
RefSeq Nucleotide NM_024827 (Hs), NM_144919 (Mm), NM_001106610 (Rn)
RefSeq Protein NP_079103 (Hs), NP_659168 (Mm), NP_001100080 (Rn)
UniProtKB Q96DB2 (Hs), Q91WA3 (Mm)
Wikipedia HDAC11 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.5.1.98

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
vorinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.4 pKi 5
⤷ pKi 7.4 (Ki 3.6x10-8 M) [5]
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 9.4 pIC50 1
⤷ pIC50 9.4 (IC50 3.7x10-10 M) [1]
fimepinostat Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.3 pIC50 3
⤷ pIC50 8.3 (IC50 5.4x10-9 M) [3]
KA1010 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.2 pIC50 2
⤷ pIC50 6.2 (IC50 5.84x10-7 M) [2]
SS-208 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 5.3 pIC50 4
⤷ pIC50 5.3 (IC50 5.12x10-6 M) [4]
Inhibitor Comments
Vorinostat has high affinity for HDACs 2, 3, 6, 9, 10 and 11, but 10-fold lower affinity for HDAC8
General Comments
HDAC11 is an atypical histone deacetylase and is the only Class IV member.

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. 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]

3. Qian C, Lai CJ, Bao R, Wang DG, Wang J, Xu GX, Atoyan R, Qu H, Yin L, Samson M et al.. (2012) Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling. Clin Cancer Res, 18 (15): 4104-13. [PMID:22693356]

4. 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]

5. Wang H, Lim ZY, Zhou Y, Ng M, Lu T, Lee K, Sangthongpitag K, Goh KC, Wang X, Wu X et al.. (2010) Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity. Bioorg Med Chem Lett, 20 (11): 3314-21. [PMID:20451378]

How to cite this page

3.5.1.- Histone deacetylases (HDACs): histone deacetylase 11. Last modified on 13/09/2019. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2615.