Reactome | PKC phosphorylates GRK2

PKC phosphorylates GRK2

Stable Identifier

R-HSA-111970

Type

Reaction [transition]

Species

Homo sapiens

Compartment

plasma membrane, cytosol

ReviewStatus

5/5

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Signal Transduction (Homo sapiens)

- Intracellular signaling by second messengers (Homo sapiens)
  - DAG and IP3 signaling (Homo sapiens)
    - CaM pathway (Homo sapiens)
      - Calmodulin induced events (Homo sapiens)
        
        PKC phosphorylates GRK2 (Homo sapiens)
- Signaling by GPCR (Homo sapiens)
  - GPCR downstream signalling (Homo sapiens)
    - G alpha (i) signalling events (Homo sapiens)
      - Opioid Signalling (Homo sapiens)
        
        G-protein mediated events (Homo sapiens)
        
        PLC beta mediated events (Homo sapiens)
        
        Ca-dependent events (Homo sapiens)
        
        CaM pathway (Homo sapiens)
        
        Calmodulin induced events (Homo sapiens)
        
        PKC phosphorylates GRK2 (Homo sapiens)

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ADRBK1 (also known as GRK2) is phosphorylated at serine 29 in vitro and in vivo by the alpha, gamma and delta isoforms of PKC. PKC-mediated phosphorylation at Ser29 increases ADRBK1 kinase activity towards GPCR substrates, contributing to GPCR desensitization. Phosphorylation at Ser29, which falls within the calmodulin-binding region of ADRBK1, abolishes the inhibitory effect of calmodulin on ADRBK1 kinase activity.

Literature References

PubMed ID	Title	Journal	Year
11042191	Phosphorylation of GRK2 by protein kinase C abolishes its inhibition by calmodulin. Krasel, C, Dammeier, S, Winstel, R, Brockmann, J, Mischak, H, Lohse, MJ	J Biol Chem	2001