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beta adrenergic receptor kinase 2

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Target id: 1467

Nomenclature: beta adrenergic receptor kinase 2

Abbreviated Name: GRK3

Family: Beta-adrenergic receptor kinases (βARKs)

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 688 22q12.1 GRK3 G protein-coupled receptor kinase 3
Mouse - 688 5 55.29 cM Grk3 G protein-coupled receptor kinase 3
Rat - 688 12q16 Grk3 G protein-coupled receptor kinase 3
Previous and Unofficial Names Click here for help
BARK2 | GRK3 | adrenergic receptor kinase, beta 2 | beta ARK2 | G-protein-coupled receptor kinase 3 | βARK2 | Adrbk2 | adrenergic
Database Links Click here for help
Alphafold P35626 (Hs), Q3UYH7 (Mm), P26819 (Rn)
BRENDA 2.7.11.15
CATH/Gene3D 2.30.29.30
ChEMBL Target CHEMBL1075166 (Hs)
Ensembl Gene ENSG00000100077 (Hs), ENSMUSG00000042249 (Mm), ENSRNOG00000059456 (Rn)
Entrez Gene 157 (Hs), 320129 (Mm), 25372 (Rn)
Human Protein Atlas ENSG00000100077 (Hs)
KEGG Enzyme 2.7.11.15
KEGG Gene hsa:157 (Hs), mmu:320129 (Mm), rno:25372 (Rn)
OMIM 109636 (Hs)
Pharos P35626 (Hs)
RefSeq Nucleotide NM_005160 (Hs), NM_177078 (Mm), NM_012897 (Rn)
RefSeq Protein NP_005151 (Hs), NP_796052 (Mm), NP_037029 (Rn)
UniProtKB P35626 (Hs), Q3UYH7 (Mm), P26819 (Rn)
Wikipedia GRK3 (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.15

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 101 [PMID: 21596927] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 4
⤷ pIC50 7.5 (IC50 3.2x10-8 M) [4]
balanol Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure 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 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
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 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 50.3
Bcr-abl inhibitor GNF-2 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 80.5
Cdc2-like kinase inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 82.9
Cdk4 inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 84.5
Cdk4 inhibitor II Small molecule or natural product Hs Inhibitor Inhibition 86.5
triciribine Small molecule or natural product Hs Inhibitor Inhibition 86.5
bisindolylmaleimide IV Small molecule or natural product Hs Inhibitor Inhibition 87.0
JNJ-7706621 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 87.2
Akt inhibitor VIII Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 87.3
AG 1295 Small molecule or natural product Hs Inhibitor Inhibition 87.4
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Antigen presentation

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 10/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1467.