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histone deacetylase 10

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Target id: 2614

Nomenclature: histone deacetylase 10

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 - 669 22q13.33 HDAC10 histone deacetylase 10
Mouse - 666 15 E3 Hdac10 histone deacetylase 10
Rat - 588 7q34 Hdac10 histone deacetylase 10
Database Links Click here for help
Alphafold Q969S8 (Hs), Q6P3E7 (Mm), Q569C4 (Rn)
BRENDA 3.5.1.98
CATH/Gene3D 3.40.800.20
ChEMBL Target CHEMBL5103 (Hs)
Ensembl Gene ENSG00000100429 (Hs), ENSMUSG00000062906 (Mm), ENSRNOG00000031915 (Rn)
Entrez Gene 83933 (Hs), 170787 (Mm), 362981 (Rn)
Human Protein Atlas ENSG00000100429 (Hs)
KEGG Enzyme 3.5.1.98
KEGG Gene hsa:83933 (Hs), mmu:170787 (Mm), rno:362981 (Rn)
OMIM 608544 (Hs)
Pharos Q969S8 (Hs)
RefSeq Nucleotide NM_032019 (Hs), NM_199198 (Mm), NM_001035000 (Rn)
RefSeq Protein NP_114408 (Hs), NP_954668 (Mm), NP_001030172 (Rn)
UniProtKB Q969S8 (Hs), Q6P3E7 (Mm), Q569C4 (Rn)
Wikipedia HDAC10 (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
bufexamac Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 4.9 pKd 2
⤷ pKd 4.9 (Kd 1.23x10-5 M) [2]
vorinostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pKi 9
⤷ pKi 7.3 (Ki 5x10-8 M) [9]
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 9.3 pIC50 1
⤷ pIC50 9.3 (IC50 4.6x10-10 M) [1]
fimepinostat Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.6 pIC50 7
⤷ pIC50 8.6 (IC50 2.8x10-9 M) [7]
CUDC-101 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 3
⤷ pIC50 7.6 (IC50 2.61x10-8 M) [3]
BML-281 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.6 pIC50 5
⤷ pIC50 7.6 (IC50 2.82x10-8 M) [5]
pracinostat Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.4 pIC50 6
⤷ pIC50 7.4 (IC50 4x10-8 M) [6]
compound 30 [PMID: 37057760] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.9 pIC50 8
⤷ pIC50 6.9 (IC50 1.273x10-7 M) [8]
KA1010 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.2 pIC50 4
⤷ pIC50 6.2 (IC50 6.43x10-7 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
HDAC10 is a Class II histone deacetylase.

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. Bantscheff M, Hopf C, Savitski MM, Dittmann A, Grandi P, Michon AM, Schlegl J, Abraham Y, Becher I, Bergamini G et al.. (2011) Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes. Nat Biotechnol, 29 (3): 255-65. [PMID:21258344]

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. 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]

5. Kozikowski AP, Tapadar S, Luchini DN, Kim KH, Billadeau DD. (2008) Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. J Med Chem, 51 (15): 4370-3. [PMID:18642892]

6. 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]

7. 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]

8. Qiu Q, Chi F, Zhou D, Xie Z, Liu Y, Wu H, Yin Z, Shi W, Qian H. (2023) Exploration of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Bispecific Inhibitors Based on the Moiety of Fedratinib for Treatment of Both Hematologic Malignancies and Solid Cancers. J Med Chem, [Epub ahead of print]. DOI: 10.1021/acs.jmedchem.3c00036 [PMID:37057760]

9. 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 10. Last modified on 18/04/2023. Accessed on 03/10/2023. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2614.