G Protein–Coupled Receptor Kinase
G protein–coupled receptor kinases (GRKs) represent a family of seven serine/threonine kinases that, based on their sequence similarities, can further be broken down into three subfamilies. These subfamilies include: GRK1, composed of GRK1 (rhodopsin kinase) and GRK7 (cone opsin kinase); GRK2, including GRK2 and GRK3; and GRK4, made up of GRK4, 5, and 6. These kinases were initially identified for their ability to phosphorylate G protein–coupled receptors (GPCRs). Phosphorylation of the receptor by GRKs leads to the recruitment of β-arrestins and consequently desensitization and internalization of the receptor. This internalization can then lead to additional signaling cascades. Furthermore, it has recently become evident that individual GRKs can interact in a kinase dependent or independent manner with nonreceptor substrates and influence a variety of physiological functions and pathologies.
Evolutionarily, GRKs are present in...
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