1.0 2018-05-07 22:21:11 UTC 2020-05-20 21:52:36 UTC BMDBP00178 Enzyme GRK5 Involved in ATP binding 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 (Beta-2 adrenergic receptor), 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) (By similarity). BMDB0001341 ADP BMDB0001429 Phosphate 26 >1773 bp ATGGAGCTGGAAAACATCGTGGCCAACACGGTCTTGCTGAAAGCCAGGGAAGGAGGCGGA GGAAAGCGCAAAGGGAAAAGCAAGAAGTGGAAGGAAATCCTGAAGTTCCCTCACATAAAC CAGTGTGAAGACCTCCGAAGAACCATAGACCGAGATTACTGCAGTTTATGTGACAAACAG CCAGTCGGGAGGCTGCTTTTCCGGCAGTTCTGCGAAACCAGACCTGGGCTGGAGTCCTAC ATTCAGTTCCTGGACTCGGTGGCAGAATATGAAGTTACTCCAGATGAAAAACTGGGAGAA AAAGGGAAGGAAATTATGACCAAGTACCTCACCCCAAAGTCCCCAGTTTTCATCACCCAA GTTGGACGGGACCTGGTCTCCCAGACGGAGGAGAAGCTCCTTCAGAAACCCTGCAAAGAA CTCTTCTCGGCCTGCGTGCAGTCTGTCCACGACTACCTGAGGGGAGAACCCTTCCACGAG TACCTGGACAGCATGTATTTTGATCGCTTTCTCCAGTGGAAGTGGTTGGAAAGGCAACCG GTAACCAAAAACACTTTCAGGCAGTACCGAGTACTAGGAAAAGGGGGCTTTGGGGAGGTC TGTGCCTGCCAGGTTCGGGCCACGGGTAAAATGTACGCCTGCAAACGCTTGGAGAAGAAG AGGATCAAAAAGAGGAAAGGGGAGTCCATGGCCCTGAATGAGAAGCAGATTCTGGAGAAG GTCAACAGTCGGTTTGTGGTCAACCTGGCCTACGCCTACGAGACCAAGGATGCCCTGTGT TTGGTCCTGACCATCATGAACGGCGGGGACCTGAAGTTCCACATTTACAACATGGGGAAC CCCGGCTTCGAGGAGGAGCGCGCCCTGTTCTACGCGGCAGAGATCCTGTGCGGCCTGGAG GACCTCCACCATGAGAACATTGTCTACAGAGATTTGAAACCTGAAAATATCCTGTTAGAC GATTACGGCCACATTAGAATTTCGGACCTGGGCCTGGCCGTGAAGATCCCCGAGGGAGAC CTGATTCGCGGCCGAGTGGGCACCGTTGGCTACATGGCTCCAGAGGTCCTGAACAACCAG AGGTATGGCCTGAGCCCCGACTACTGGGGTCTGGGCTGCCTCATCTACGAGATGATCGAG GGCCAGTCGCCCTTCCGCGGCCGCAAGGAGAAGGTGAAGCGGGAGGAGGTGGACCGCCGG GTGTTGGAGACAGAGGAGGTGTACTCGCACAAGTTCTCCGAGGAGGCCAAGTCCATCTGC AAAATGCTGCTCACCAAAGATGCAAAGCAGAGGCTGGGCTGCCAGGAGGAAGGGGCCGCG GAGGTCAAGAGACACCCCTTCTTCAGGAACATGAATTTCAAGCGCTTAGAGGCCGGGATG TTGGATCCCCCCTTTGTTCCAGATCCCCGGGCCGTGTACTGCAAGGACGTCTTGGACATC GAGCAGTTCTCCACCGTGAAGGGCGTCAACCTGGACCACACGGACGACGACTTCTACTCC AAGTTCTCCACGGGCTCTGTGCCCATCCCGTGGCAAAGCGAGATGATAGAAACAGAGTGC TTTAAGGAGCTGAACGTGTTCGGACCCCACGGTACCCTCTCACCGGACCTGAACCGAAGC CACCCTCCGGAACCGCCAAAGAAAGGGCTGCTCCAGAGGCTCTTCAAGCGTCAGCATCAA AACAATTCCAAGAGTTCACCCAATTCCAAGACCAGTTTTAACCACCACATCAATTCAAAC CACGTGAGTTCAAACTCCACCGGAAGCAGCTAG 590 67889.0 8.32 25-45 55-75 109-129 141-162 168-186 198-218 255-273 284-304 308-328 None >G protein-coupled receptor kinase 5 MELENIVANTVLLKAREGGGGKRKGKSKKWKEILKFPHINQCEDLRRTIDRDYCSLCDKQ PVGRLLFRQFCETRPGLESYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFITQ VGRDLVSQTEEKLLQKPCKELFSACVQSVHDYLRGEPFHEYLDSMYFDRFLQWKWLERQP VTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKRLEKKRIKKRKGESMALNEKQILEK VNSRFVVNLAYAYETKDALCLVLTIMNGGDLKFHIYNMGNPGFEEERALFYAAEILCGLE DLHHENIVYRDLKPENILLDDYGHIRISDLGLAVKIPEGDLIRGRVGTVGYMAPEVLNNQ RYGLSPDYWGLGCLIYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSIC KMLLTKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYCKDVLDI EQFSTVKGVNLDHTDDDFYSKFSTGSVPIPWQSEMIETECFKELNVFGPHGTLSPDLNRS HPPEPPKKGLLQRLFKRQHQNNSKSSPNSKTSFNHHINSNHVSSNSTGSS AAA17561.1 P43249 GRK5_BOVIN 4WNK 4WNK U01206 GRK5