histone deacetylase 10

Target id: 2614

Nomenclature: histone deacetylase 10

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 10 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 669 22q13.31 HDAC10 histone deacetylase 10
Mouse - 666 15 E3 Hdac10 histone deacetylase 10
Rat - 588 7q34 Hdac10 histone deacetylase 10
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
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
bufexamac Hs Inhibition 4.9 pKd 2
pKd 4.9 (Kd 1.23x10-5 M) [2]
vorinostat Hs Inhibition 7.3 pKi 6
pKi 7.3 (Ki 5x10-8 M) [6]
quisinostat Hs Inhibition 9.3 pIC50 1
pIC50 9.3 (IC50 4.6x10-10 M) [1]
CUDC-907 Hs Inhibition 8.6 pIC50 5
pIC50 8.6 (IC50 2.8x10-9 M) [5]
CUDC-101 Hs Inhibition 7.6 pIC50 3
pIC50 7.6 (IC50 2.61x10-8 M) [3]
pracinostat Hs Inhibition 7.4 pIC50 4
pIC50 7.4 (IC50 4x10-8 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. 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]

5. 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]

6. 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 11/12/2015. Accessed on 23/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2614.