beta adrenergic receptor kinase 2 | Beta-adrenergic receptor kinases (βARKs) | IUPHAR/BPS Guide to PHARMACOLOGY

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beta adrenergic receptor kinase 2

Target not currently curated in GtoImmuPdb

Target id: 1467

Nomenclature: beta adrenergic receptor kinase 2

Abbreviated Name: GRK3

Family: Beta-adrenergic receptor kinases (βARKs)

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 688 22q11 GRK3 G protein-coupled receptor kinase 3
Mouse - 688 5 Grk3 G protein-coupled receptor kinase 3
Rat - 688 12q16 Grk3 G protein-coupled receptor kinase 3
Previous and Unofficial Names
BARK2 | GRK3 | adrenergic receptor kinase, beta 2 | beta ARK2 | G-protein-coupled receptor kinase 3 | βARK2 | Adrbk2 | adrenergic
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.15

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 Value Parameter Reference
compound 101 [PMID: 21596927] Hs Inhibition 7.5 pIC50 4
pIC50 7.5 (IC50 3.2x10-8 M) [4]
balanol Hs Inhibition 7.3 pIC50 3
pIC50 7.3 (IC50 4.7x10-8 M) [3]
Inhibitor Comments
A component of agonist-induced desensitisation of the μ opioid receptor is reversed by compound 101 inhibition of GRK2/3 [2].
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/GRK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Hs Inhibitor Inhibition 50.3
Bcr-abl inhibitor GNF-2 Hs Inhibitor Inhibition 80.5
Cdc2-like kinase inhibitor Hs Inhibitor Inhibition 82.9
Cdk4 inhibitor III Hs Inhibitor Inhibition 84.5
triciribine Hs Inhibitor Inhibition 86.5
Cdk4 inhibitor II Hs Inhibitor Inhibition 86.5
bisindolylmaleimide IV Hs Inhibitor Inhibition 87.0
JNJ-7706621 Hs Inhibitor Inhibition 87.2
Akt inhibitor VIII Hs Inhibitor Inhibition 87.3
AG 1295 Hs Inhibitor Inhibition 87.4
Displaying the top 10 most potent ligands  View all ligands in screen »

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. Lowe JD, Sanderson HS, Cooke AE, Ostovar M, Tsisanova E, Withey SL, Chavkin C, Husbands SM, Kelly E, Henderson G et al.. (2015) Role of G Protein-Coupled Receptor Kinases 2 and 3 in μ-Opioid Receptor Desensitization and Internalization. Mol. Pharmacol., 88 (2): 347-56. [PMID:26013542]

3. Tesmer JJ, Tesmer VM, Lodowski DT, Steinhagen H, Huber J. (2010) Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol. J. Med. Chem., 53 (4): 1867-70. [PMID:20128603]

4. Thal DM, Yeow RY, Schoenau C, Huber J, Tesmer JJ. (2011) Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol. Pharmacol., 80 (2): 294-303. [PMID:21596927]

How to cite this page

Beta-adrenergic receptor kinases (βARKs): beta adrenergic receptor kinase 2. Last modified on 10/06/2015. Accessed on 12/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1467.