Beta-adrenergic receptor kinases (βARKs)

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Kinases (EC 2.7.x.x)
AGC: Containing PKA, PKG, PKC families
G protein-coupled receptor kinases (GRKs)
Beta-adrenergic receptor kinases (βARKs)

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Enzymes

GRK2 (beta adrenergic receptor kinase 1) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1466

Nomenclature

beta adrenergic receptor kinase 1

Common abbreviation

GRK2

Previous and unofficial names

Genes

GRK2 (Hs), Grk2 (Mm), Grk2 (Rn)

Ensembl ID

ENSG00000173020 (Hs), ENSMUSG00000024858 (Mm), ENSRNOG00000018985 (Rn)

UniProtKB AC

P25098 (Hs), Q99MK8 (Mm), P26817 (Rn)

EC number

2.7.11.15

Inhibitors

CCG258747 pIC₅₀ 7.7 [1]

Comment

Protein kinase C-mediated phosphorylation increases membrane association [2-3]

GRK3 (beta adrenergic receptor kinase 2) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1467

Nomenclature

beta adrenergic receptor kinase 2

Common abbreviation

GRK3

Previous and unofficial names

Genes

GRK3 (Hs), Grk3 (Mm), Grk3 (Rn)

Ensembl ID

ENSG00000100077 (Hs), ENSMUSG00000042249 (Mm), ENSRNOG00000059456 (Rn)

UniProtKB AC

P35626 (Hs), Q3UYH7 (Mm), P26819 (Rn)

EC number

2.7.11.15

References

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1. Bouley RA, Weinberg ZY, Waldschmidt HV, Yen YC, Larsen SD, Puthenveedu MA, Tesmer JJG. (2020) A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of the μ-Opioid Receptor. Mol Pharmacol, 97 (6): 392-401. [PMID:32234810]

2. Chuang TT, LeVine H, De Blasi A. (1995) Phosphorylation and activation of beta-adrenergic receptor kinase by protein kinase C. J Biol Chem, 270 (31): 18660-5. [PMID:7629197]

3. Winstel R, Freund S, Krasel C, Hoppe E, Lohse MJ. (1996) Protein kinase cross-talk: membrane targeting of the beta-adrenergic receptor kinase by protein kinase C. Proc Natl Acad Sci USA, 93 (5): 2105-9. [PMID:8700892]

How to cite this family page

Database page citation:

Beta-adrenergic receptor kinases (βARKs). Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=507.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.