GRK5 - G protein-coupled receptor kinase 5 - human protein (Function)
 
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GRK5 »  G protein-coupled receptor kinase 5   [ EC 2.7.11.16 ]
 
Protein also known as:  G protein-coupled receptor kinase GRK5.
Gene name:  GRK5
Entry whose protein(s) existence is based on evidence at protein level
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GENE REF ISO

Function

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Overview 
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).  
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  • CuratedUniProtKB
GO molecular function 
ATP bindingdefinition[GO:0005524]  
  • IEAUniProtKB KW
G-protein coupled receptor kinase activitydefinition[GO:0004703]  
  • IEAEC 2 GO
Phospholipid bindingdefinition[GO:0005543]  
1
  • TASPINC
Protein bindingdefinition[GO:0005515]  
3
  • IPIUniProtKB
  • IPIIntAct
  • IPIBHF-UCL
Protein kinase C bindingdefinition[GO:0005080]  
1
  • TASPINC
Protein serine/threonine kinase activitydefinition[GO:0004674]  
1
  • IDAUniProtKB
GO biological process 
Adenylate cyclase-modulating G-protein coupled receptor signaling pathwaydefinition[GO:0007188]  
1
  • TASPINC
Apoptotic processdefinition[GO:0006915]  
  • IEAUniProtKB KW
Negative regulation of apoptotic processdefinition[GO:0043066]  
1
  • IDAUniProtKB
Protein autophosphorylationdefinition[GO:0046777]  
1
  • IDAUniProtKB
Regulation of G-protein coupled receptor protein signaling pathwaydefinition[GO:0008277]  
1
  • TASPINC
Tachykinin receptor signaling pathwaydefinition[GO:0007217]  
1
  • IDABHF-UCL
Termination of G-protein coupled receptor signaling pathwaydefinition[GO:0038032] silver  
  • IEAInterPro 2 GO
Wnt signaling pathwaydefinition[GO:0016055]  
  • IEAUniProtKB KW
Enzymatic activity 
This protein acts as an enzyme. It is known to catalyze the following reaction
EC 2.7.11.16: ATP + [G-protein-coupled receptor] ADP + [G-protein-coupled receptor] phosphate.  
  • CuratedUniProtKB
It is regulated in the following manner
Inhibited by calmodulin with an IC(50) of 50 nM. Calmodulin inhibits GRK5 association with receptor and phospholipid.  
1
  • CuratedUniProtKB
 
More information is available from:
Pathways 
According to KEGG, this protein belongs to the following pathways:
Chemokine signaling pathway  hsa04062+2869  
Endocytosis  hsa04144+2869  
According to Reactome, this protein belongs to the following pathway:
G alpha (q) signalling events  REACT_18283  
 

Keywords

Biological process 
Apoptosis  definition   [KW-0053]
Wnt signaling pathway  definition   [KW-0879]
Molecular function 
Kinase  definition   [KW-0418]
Serine/threonine-protein kinase  definition   [KW-0723]
Transferase  definition   [KW-0808]
Technical term 
Reference proteome  definition   [KW-1185]
 

Further external links

Other
GeneWiki: GRK5
GenomeRNAi: 2869
PRO: PR:P34947
Chemistry
GuidetoPHARMACOLOGY: 1469