| Tissue Specificity | Highest levels in heart, placenta, lung > skeletal muscle > brain, liver, pancreas > kidney. |
| Post Translational Modifications | Autophosphorylated. Autophosphorylation may play a critical role in the regulation of GRK5 kinase activity. |
| Function | 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). |
| Protein Name | G Protein-Coupled Receptor Kinase 5G Protein-Coupled Receptor Kinase Grk5 |
| Database Links | Reactome: R-HSA-416476Reactome: R-HSA-418555 |
| Cellular Localisation | CytoplasmNucleusCell MembranePeripheral Membrane ProteinPredominantly Localized At The Plasma MembraneTargeted To The Cell Surface Through The Interaction With PhospholipidsNucleus Localization Is Regulated In A Gpcr And Ca(2+)/Calmodulin-Dependent Fashion |
| Alternative Antibody Names | Anti-G Protein-Coupled Receptor Kinase 5 antibodyAnti-G Protein-Coupled Receptor Kinase Grk5 antibodyAnti-GRK5 antibodyAnti-GPRK5 antibody |
Information sourced from Uniprot.org
