Multiple pathways of rapid beta 2-adrenergic receptor desensitization. Delineation with specific inhibitors.

MJ Lohse, JL Benovic, MG Caron… - Journal of Biological …, 1990 - ASBMB
Exposure of beta-adrenergic receptors (beta ARs) to agonists causes rapid desensitization
of the receptor-stimulated adenylyl cyclase response. Three main mechanisms have been
implicated in this process: phosphorylation of the receptors by the cAMP-dependent protein
kinase (PKA), phosphorylation by the specific agonist-dependent beta AR kinase, and
sequestration of the receptors away from the cell surface. By applying inhibitors of these
processes to digitonin-permeabilized A431 cells we investigated their contributions to beta …