A G protein-coupled receptor kinase 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P34947]
EC 2.7.11.16;
G protein-coupled receptor kinase GRK5
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 5 (83.33) | 24.3611 |
| 2020's | 1 (16.67) | 2.80 |
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| paroxetine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0490 | 2 | 2 |
| birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| ophiocordin | Homo sapiens (human) | IC50 | 0.1600 | 1 | 1 |
| su 11248 | Homo sapiens (human) | IC50 | 0.8300 | 1 | 1 |
This protein enables 8 target(s):
| Target | Category | Definition |
|---|---|---|
| protein serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
| G protein-coupled receptor kinase activity | molecular function | Catalysis of the reaction: ATP + G protein-coupled receptor = ADP + G protein-coupled receptor phosphate. [GOC:dph] |
| protein kinase C binding | molecular function | Binding to protein kinase C. [GOC:jl] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| phospholipid binding | molecular function | Binding to a phospholipid, a class of lipids containing phosphoric acid as a mono- or diester. [ISBN:0198506732] |
| beta-adrenergic receptor kinase activity | molecular function | Catalysis of the reaction: ATP + beta-adrenergic receptor = ADP + phospho-beta-adrenergic receptor. [EC:2.7.11.15, MetaCyc:BETA-ADRENERGIC-RECEPTOR-KINASE-RXN] |
| protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|---|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| nuclear speck | cellular component | A discrete extra-nucleolar subnuclear domain, 20-50 in number, in which splicing factors are seen to be localized by immunofluorescence microscopy. [http://www.cellnucleus.com/] |
| nuclear membrane | cellular component | Either of the lipid bilayers that surround the nucleus and form the nuclear envelope; excludes the intermembrane space. [GOC:mah, GOC:pz] |
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|---|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
This protein is involved in 13 target(s):
| Target | Category | Definition |
|---|---|---|
| apoptotic process | biological process | A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of adenylyl cyclase activity and a subsequent change in the intracellular concentration of cyclic AMP (cAMP). [GOC:mah, GOC:signaling, ISBN:0815316194] |
| tachykinin receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by tachykinin binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. Tachykinin is a short peptide with the terminal sequence (Phe-X-Gly-Leu-Met-NH2). [GOC:mah, PMID:14723970] |
| regulation of G protein-coupled receptor signaling pathway | biological process | Any process that modulates the frequency, rate or extent of G protein-coupled receptor signaling pathway. [GOC:go_curators] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| Wnt signaling pathway | biological process | The series of molecular signals initiated by binding of a Wnt protein to a frizzled family receptor on the surface of a target cell and ending with a change in cell state. [PMID:11532397] |
| negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| fat cell differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of an adipocyte, an animal connective tissue cell specialized for the synthesis and storage of fat. [CL:0000136, GOC:go_curators] |
| protein autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732] |
| regulation of cell cycle | biological process | Any process that modulates the rate or extent of progression through the cell cycle. [GOC:ai, GOC:dph, GOC:tb] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| regulation of signal transduction | biological process | Any process that modulates the frequency, rate or extent of signal transduction. [GOC:sm] |