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casein kinase 2, alpha prime polypeptide subunit

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 1550

Nomenclature: casein kinase 2, alpha prime polypeptide subunit

Abbreviated Name: CK2-A2

Family: Casein kinase 2 (CK2) family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 350 16q21 CSNK2A2 casein kinase 2 alpha 2
Mouse - 350 8 Csnk2a2 casein kinase 2, alpha prime polypeptide
Rat - 350 19p13 Csnk2a2 casein kinase 2 alpha 2
Previous and Unofficial Names Click here for help
casein kinase 2
Database Links Click here for help
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of a human CK2alpha prime, the paralog isoform of the catalytic subunit of protein kinase CK2 from Homo sapiens
PDB Id:  3OFM
Resolution:  2.0Å
Species:  Human
References:  2
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

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
compound 2c [PMID: 22115617] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pKi 6
pKi 7.7 (Ki 2.1x10-8 M) [6]
silmitasertib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.0 pIC50 7
pIC50 9.0 (IC50 1x10-9 M) [7]
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 3,8

Key to terms and symbols Click column headers to sort
Target used in screen: CSNK2A2
Ligand Sp. Type Action Value Parameter
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.5 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0 pKd
GSK-461364A Small molecule or natural product Hs Inhibitor Inhibition 6.0 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: CK2α2/CK2a2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PI 3-Kg inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.1 -12.0 -5.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 4.5 63.0 49.0
STO609 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 13.3 18.0 4.0
GSK-3 inhibitor XIII Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 15.0 21.0 -2.0
casein kinase II inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 17.0 33.0 5.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 22.0 12.0 -1.0
JNK inhibitor V Small molecule or natural product Hs Inhibitor Inhibition 27.1 41.0 15.0
indirubin derivative E804 Small molecule or natural product Hs Inhibitor Inhibition 28.3 46.0 3.0
PI 3-Kg inhibitor II Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 29.9 52.0 0.0
PKR inhibitor, negative control Small molecule or natural product Hs Inhibitor Inhibition 33.3 92.0 32.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
CSNK2A2 is included in Guide to IMMUNOPHARMACOLOGY as it is a subunit of the casein kinase 2 complex.
General Comments
SARS-CoV-2/COVID-19
Experimental in vitro evidence, using affinity-purification mass spectrometry (AP-MS), indicates a protein-protein interaction between CSNK2A2 and the SARS-CoV-2 nucleocapsid phosphoprotein (N) [5], although whether this interaction is realistic based on spatial distribution of the host and viral proteins within cells was not addressed in this study. Speculatively,CSNK2A2 ligands such as silmitasertib or TMCB could be utilised to examine the effect of inhibiting the CSNK2A2-N protein-protein interaction on SARS-CoV-2 pathobiology.

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. Bischoff N, Olsen B, Raaf J, Bretner M, Issinger OG, Niefind K. (2011) Structure of the human protein kinase CK2 catalytic subunit CK2α' and interaction thermodynamics with the regulatory subunit CK2β. J. Mol. Biol., 407 (1): 1-12. [PMID:21241709]

3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

5. Gordon DE, Jang GM, Bouhaddou M, Xu J, Obernier K, White KM, O'Meara MJ, Rezelj VV, Guo JZ, Swaney DL et al.. (2020) A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. Nature, [Epub ahead of print]. [PMID:32353859]

6. Janeczko M, Orzeszko A, Kazimierczuk Z, Szyszka R, Baier A. (2012) CK2α and CK2α' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives. Eur J Med Chem, 47 (1): 345-50. [PMID:22115617]

7. Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E et al.. (2011) Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. J. Med. Chem., 54 (2): 635-54. [PMID:21174434]

8. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Casein kinase 2 (CK2) family: casein kinase 2, alpha prime polypeptide subunit. Last modified on 27/03/2020. Accessed on 27/10/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1550.