VRK serine/threonine kinase 2 | Vaccina related kinase (VRK) family | IUPHAR/BPS Guide to PHARMACOLOGY

VRK serine/threonine kinase 2

Target id: 2276

Nomenclature: VRK serine/threonine kinase 2

Abbreviated Name: VRK2

Family: Vaccina related kinase (VRK) family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for VRK serine/threonine kinase 2 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 508 2p16.1 VRK2 VRK serine/threonine kinase 2
Mouse - 503 11 A3.3 Vrk2 vaccinia related kinase 2
Rat - 229 14 q22 Vrk2 VRK serine/threonine kinase 2
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of VRK2.
PDB Id:  2V62
Resolution:  1.7Å
Species:  Human
References:  3
Enzyme Reaction
EC Number: 2.7.11.1
DiscoveRx KINOMEscan® screen
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: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: VRK2
Ligand Sp. Type Action Affinity Units
alvocidib Hs Inhibitor Inhibition 7.2 pKd
bosutinib Hs Inhibitor Inhibition 6.2 pKd
erlotinib Hs Inhibitor Inhibition <5.5 pKd
GSK690693 Hs Inhibitor Inhibition <5.5 pKd
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd
SB203580 Hs Inhibitor Inhibition <5.5 pKd
masitinib Hs Inhibitor Inhibition <5.5 pKd
gefitinib Hs Inhibitor Inhibition <5.5 pKd
crizotinib Hs Inhibitor Inhibition <5.5 pKd
staurosporine Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
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: 2...

Key to terms and symbols Click column headers to sort
Target used in screen: VRK2/nd
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
indirubin derivative E804 Hs Inhibitor Inhibition 69.0 26.0
compound 52 [PMID: 9677190] Hs Inhibitor Inhibition 71.0 19.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 71.0 28.0
Flt-3 inhibitor II Hs Inhibitor Inhibition 72.0 37.0
PKR inhibitor Hs Inhibitor Inhibition 75.0 26.0
Cdk1 inhibitor Hs Inhibitor Inhibition 76.0 28.0
SP600125 Hs Inhibitor Inhibition 78.0 36.0
Cdk2 inhibitor III Hs Inhibitor Inhibition 79.0 46.0
JAK3 inhibitor II Hs Inhibitor Inhibition 83.0 56.0
IC261 Hs Inhibitor Inhibition 83.0 32.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

1. 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]

2. 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]

3. Scheeff ED, Eswaran J, Bunkoczi G, Knapp S, Manning G. (2009) Structure of the pseudokinase VRK3 reveals a degraded catalytic site, a highly conserved kinase fold, and a putative regulatory binding site. Structure, 17 (1): 128-38. [PMID:19141289]

4. 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

Vaccina related kinase (VRK) family: VRK serine/threonine kinase 2. Last modified on 18/09/2018. Accessed on 26/09/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2276.