GRK2 was originally identified as a protein kinase that phosphorylated the β2-adrenergic receptor, and has been most extensively studied as a regulator of adrenergic receptors (and other GPCRs) in the heart, where it has been proposed as a drug target to treat heart failure.

Aug 2, 2023 · Here we report the complex structure of neurotensin receptor 1 (NTSR1) bound to GRK2, Gαq and the arrestin-biased ligand SBI-5537.

Oct 27, 2016 · G-protein-coupled receptor kinase 2 (GRK2) is a G-protein-coupled receptor kinase that is ubiquitously expressed in many tissues and regulates various intracellular mechanisms. The up- or down-regulation of GRK2 correlates with several pathological disorders.

GRK2 is a critical regulator of immune cell signaling, influencing the functional dynamics of various immune cell populations and their interactions within the tumor microenvironment. Dysregulation of GRK2 has been implicated in the etiology of several autoimmune disorders, including RA, IBD, and MS, where it disrupts immune homeostasis and ...

GRK2 was first identified as an enzyme that phosphorylated the beta-2 adrenergic receptor, and was originally called the beta adrenergic receptor kinase (βARK, or ββARK1). GRK2 is overexpressed in heart failure, and GRK2 inhibition could be used to …

Emerging evidence suggests that GRK2, the most widely studied member of this family of kinases, modulates multiple cellular responses in various physiological contexts by either phosphorylating non-receptor substrates or by directly interacting with signaling molecules.

Mar 5, 2025 · GRK2 is a particularly significant member of the GRK family. Recent studies have demonstrated that GRK2 primarily regulates immune cell function and homeostasis through receptor desensitization. Over the past decade, substantial progress has been made in elucidating the role of GRK2 in various human diseases. Notably, GRK2 is implicated in a ...

Mar 30, 2025 · GRK2 (G Protein-Coupled Receptor Kinase 2) is a Protein Coding gene. Diseases associated with GRK2 include Short-Rib Thoracic Dysplasia 1 With Or Without Polydactyly and Asphyxiating Thoracic Dystrophy .

Feb 8, 2025 · GRK2-phosphorylated recombinant ribosomal protein P2 reconstitutes translational activity of 60S ribosomal subunits and represents a potential novel signaling pathway responsible for P2 phosphorylation. GRK2 is potential marker for organ injury and survival after cardiopulmonary bypass

G protein–coupled receptor kinase 2 (GRK2) plays a central role in G protein–coupled receptor regulation. Recent research is uncovering its involvement in additional cellular functions, but the potential role of GRK2 in the cell cycle has not been addressed.