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Target not currently curated in GtoImmuPdb
Target id: 1467
Nomenclature: beta adrenergic receptor kinase 2
Abbreviated Name: GRK3
Gene and Protein Information | ||||||
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 |
BARK2 | GRK3 | beta ARK2 | adrenergic receptor kinase, beta 2 | G-protein-coupled receptor kinase 3 | βARK2 | Adrbk2 | adrenergic |
Database Links | |
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 | ||||
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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 |
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Key to terms and symbols | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Target used in screen: nd/GRK3 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immuno Process Associations | ||
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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]
Beta-adrenergic receptor kinases (βARKs): beta adrenergic receptor kinase 2. Last modified on 10/06/2015. Accessed on 08/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1467.