Historical Background
G-protein coupled receptor kinase 2 (GRK2) was first discovered in 1989 by Benovic et al. as a 79.7 kDa protein that can specifically phosphorylate the agonist-occupied form of the β2-adrenergic receptor, hence the name β-adrenergic receptor kinase 1. Based on sequence homology and structural similarity, GRK2 is grouped with six other GRKs into a family of serine/threonine protein kinases that phosphorylate and regulate activated G-protein-coupled receptors (GPCRs). GRK2 has well-established roles in the cardiovascular system, nervous system, liver, and immune cells. Altered GRK2 expression has been reported in several disorders including heart failure, opioid addiction, multiple sclerosis, rheumatoid arthritis, major depression, schizophrenia, bipolar disorder, and Parkinson’s disease.
Structure, Expression, and Function
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Cheng, A.H.H., Cheng, HY.M. (2018). GRK2 (G Protein-Coupled Receptor Kinase 2). In: Choi, S. (eds) Encyclopedia of Signaling Molecules. Springer, Cham. https://doi.org/10.1007/978-3-319-67199-4_101765
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