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  • Title: Phorbol-ester-induced phosphorylation of the beta 2-adrenergic receptor decreases its coupling to Gs.
    Author: Bouvier M, Guilbault N, Bonin H.
    Journal: FEBS Lett; 1991 Feb 25; 279(2):243-8. PubMed ID: 1848190.
    Abstract:
    Phorbol-esters have been shown to modulate the beta-adrenergic-stimulated adenylyl cyclase in a number of cell lines. Here, using site directed mutagenesis, we investigate the role of the beta 2-adrenergic receptor phosphorylation by protein kinase C in this regulatory process. Mutation of the serine-261, -262, -344 and -345 of the beta 2-adrenergic receptor prevented the phorbol-ester-induced phosphorylation of the receptor. This mutation also abolished the phorbol-ester-induced decrease in high-affinity agonist binding and potency of the beta 2-adrenergic receptor. We suggest that protein kinase C mediated phosphorylation of the receptor promotes its functional uncoupling.
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