Phorbol-ester-induced phosphorylation of the beta 2-adrenergic receptor decreases its coupling to Gs.

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.

journal_name

FEBS Lett

journal_title

FEBS letters

authors

Bouvier M,Guilbault N,Bonin H

doi

10.1016/0014-5793(91)80159-z

subject

Has Abstract

pub_date

1991-02-25 00:00:00

pages

243-8

issue

2

eissn

0014-5793

issn

1873-3468

pii

0014-5793(91)80159-Z

journal_volume

279

pub_type

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