======= 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 |}}