======= GRK5 ======= == Gene Information == * **Official Symbol**: GRK5 * **Official Name**: G protein-coupled receptor kinase 5 * **Aliases and Previous Symbols**: N/A * **Entrez ID**: [[https://www.ncbi.nlm.nih.gov/gene/?term=2869|2869]] * **UniProt**: [[https://www.uniprot.org/uniprot/P34947|P34947]] * **Interactions**: [[https://thebiogrid.org/search.php?search=GRK5&organism=9606|BioGRID]] * **PubMed articles**: [[https://www.ncbi.nlm.nih.gov/pubmed/?term=gene%20GRK5|Open PubMed]] * **OMIM**: [[https://omim.org/entry/600870|Open OMIM]] == Function Summary == * **Entrez Summary**: N/A * **UniProt Summary**: 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). {ECO:0000269|PubMed:19661922, ECO:0000269|PubMed:19801552, ECO:0000269|PubMed:20038610, ECO:0000269|PubMed:20124405, ECO:0000269|PubMed:21728385}. |Pkinase Tyr| |RGS| |Pkinase| |beta-adrenergic receptor kinase activity| |G protein-coupled receptor kinase activity| |tachykinin receptor signaling pathway| |protein kinase C binding| |phospholipid binding| |fat cell differentiation| |regulation of G protein-coupled receptor signaling pathway| |protein autophosphorylation| |adenylate cyclase-modulating G protein-coupled receptor signaling pathway| |nuclear membrane| |G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger| |Wnt signaling pathway| |cell-cell signaling by wnt| |protein serine/threonine kinase activity| |nuclear speck| |cell surface receptor signaling pathway involved in cell-cell signaling| |negative regulation of apoptotic process| |negative regulation of programmed cell death| |positive regulation of cell population proliferation| |apoptotic process| |protein phosphorylation| |negative regulation of cell death| |programmed cell death| |cell death| |cell-cell signaling| |regulation of cell cycle| |phosphorylation| |G protein-coupled receptor signaling pathway| |ATP binding| |regulation of apoptotic process| |regulation of programmed cell death| |regulation of cell population proliferation| |regulation of cell death| \\ === CRISPR Data === ^Screen^Score^ |[[:results:exp6|Bortezomib 0.005μM R00 exp6]]|-1.89| |[[:results:exp143|Phenformin 20μM R03 exp143]]|-1.7| |[[:results:exp58|UM131593 0.1μM R01 exp58]]|1.73| |[[:results:exp12|Chloramphenicol 2μM R00 exp12]]|1.82| No correlation found to any other genes in chemogenomics. Global Fraction of Cell Lines Where Essential: 0/739 ^Tissue^Fraction Of Cell Lines Where Essential^ |1290807.0|0/1| |909776.0|0/1| |bile duct|0/28| |blood|0/28| |bone|0/26| |breast|0/33| |central nervous system|0/56| |cervix|0/4| |colorectal|0/17| |esophagus|0/13| |fibroblast|0/1| |gastric|0/16| |kidney|0/21| |liver|0/20| |lung|0/75| |lymphocyte|0/16| |ovary|0/26| |pancreas|0/24| |peripheral nervous system|0/16| |plasma cell|0/15| |prostate|0/1| |skin|0/24| |soft tissue|0/9| |thyroid|0/2| |upper aerodigestive|0/22| |urinary tract|0/29| |uterus|0/5| == Essentiality in NALM6 == * **Essentiality Rank**: 11076 * **Expression level (log2 read counts)**: 3.11 {{:chemogenomics:nalm6 dist.png?nolink |}}