GRK5
Entrez ID: 2869
Full name: G protein-coupled receptor kinase 5
External links: HGNC UniprotKB Ensembl RefSeq COSMIC
Family: AGC: GRK: GRK
Chromosomal location: 10q26.11
Substructure location: Gatekeeper: 263 A-loop: 328...350 G-loop: 193...200 αC-helix: 219...224
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GRK5
Serine/threonine kinase that phosphorylates preferentially the activated forms of a variety of G-protein-coupled receptors (GPCRs). Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their down-regulation. Phospho...
Serine/threonine kinase that phosphorylates preferentially the activated forms of a variety of G-protein-coupled receptors (GPCRs). Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their down-regulation. Phosphorylates a variety of GPCRs, including adrenergic receptors, muscarinic acetylcholine receptors (more specifically Gi-coupled M2/M4 subtypes), dopamine receptors and opioid receptors. In addition to GPCRs, also phosphorylates various substrates: Hsc70-interacting protein/ST13, TP53/p53, HDAC5, and arrestin-1/ARRB1. Phosphorylation of ARRB1 by GRK5 inhibits G-protein independent MAPK1/MAPK3 signaling downstream of 5HT4-receptors. Phosphorylation of HDAC5, a repressor of myocyte enhancer factor 2 (MEF2) leading to nuclear export of HDAC5 and allowing MEF2-mediated transcription. Phosphorylation of TP53/p53, a crucial tumor suppressor, inhibits TP53/p53-mediated apoptosis. Phosphorylation of ST13 regulates internalization of the chemokine receptor. Phosphorylates rhodopsin (RHO) (in vitro) and a non G-protein-coupled receptor, LRP6 during Wnt signaling (in vitro).
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GO - Biological processes (BP):
adenylate cyclase-modulating G protein-coupled receptor signaling pathway, apoptotic process, fat cell differentiation, G protein-coupled receptor signaling pathway, negative regulation of apoptotic process, positive regulation of cell population proliferation, protein autophosphorylation, regulatio...
adenylate cyclase-modulating G protein-coupled receptor signaling pathway, apoptotic process, fat cell differentiation, G protein-coupled receptor signaling pathway, negative regulation of apoptotic process, positive regulation of cell population proliferation, protein autophosphorylation, regulation of cell cycle, regulation of G protein-coupled receptor signaling pathway, tachykinin receptor signaling pathway, Wnt signaling pathway
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GO - Molecular function (MF):
ATP binding, beta-adrenergic receptor kinase activity, G protein-coupled receptor kinase activity, phospholipid binding, protein kinase C binding, protein serine/threonine kinase activity...
ATP binding, beta-adrenergic receptor kinase activity, G protein-coupled receptor kinase activity, phospholipid binding, protein kinase C binding, protein serine/threonine kinase activity
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GO - Cellular component (CC):
cytosol, nuclear membrane, nuclear speck, plasma membrane, cytoplasm...
cytosol, nuclear membrane, nuclear speck, plasma membrane, cytoplasm
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G protein-coupled receptor kinase 5
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Kaplan plot for GRK5 in
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*NOTE: the Kaplan plots were collected from OncoLnc