VRK serine/threonine kinase 1 | Vaccina related kinase (VRK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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VRK serine/threonine kinase 1

Target id: 2275

Nomenclature: VRK serine/threonine kinase 1

Abbreviated Name: VRK1

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 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 396 14q32.2 VRK1 VRK serine/threonine kinase 1
Mouse - 416 12 F1 Vrk1 vaccinia related kinase 1
Rat - 414 6 q32 Vrk1 VRK serine/threonine kinase 1
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  NMR solution structure of human Vaccinia-Related Kinase 1.
PDB Id:  2LAV
Resolution:  0.0Å
Species:  Human
References:  2
Enzyme Reaction
EC Number: 2.7.11.1
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: ...1

Key to terms and symbols Click column headers to sort
Target used in screen: nd/VRK1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PKR inhibitor Hs Inhibitor Inhibition 69.1
Gö 6983 Hs Inhibitor Inhibition 76.7
PDGF receptor tyrosine kinase inhibitor III Hs Inhibitor Inhibition 77.4
isogranulatimide Hs Inhibitor Inhibition 78.1
H-89 Hs Inhibitor Inhibition 80.1
K-252a Hs Inhibitor Inhibition 80.5
PKR inhibitor, negative control Hs Inhibitor Inhibition 80.6
GSK-3 inhibitor X Hs Inhibitor Inhibition 80.7
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 81.0
TWS119 Hs Inhibitor Inhibition 81.6
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Pontocerebellar hypoplasia type 1A; PCH1A
Disease Ontology: DOID:0060265
OMIM: 607596
Orphanet: ORPHA2254

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. Shin J, Chakraborty G, Bharatham N, Kang C, Tochio N, Koshiba S, Kigawa T, Kim W, Kim KT, Yoon HS. (2011) NMR solution structure of human vaccinia-related kinase 1 (VRK1) reveals the C-terminal tail essential for its structural stability and autocatalytic activity. J. Biol. Chem., 286 (25): 22131-8. [PMID:21543316]

How to cite this page

Vaccina related kinase (VRK) family: VRK serine/threonine kinase 1. Last modified on 18/09/2018. Accessed on 21/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2275.