[HTML][HTML] α2A/α2C-adrenergic receptor third loop chimera show that agonist interaction with receptor subtype backbone establishes G protein-coupled receptor kinase …

EA Jewell-Motz, KM Small, CT Theiss… - Journal of Biological …, 2000 - ASBMB
The α 2A-adrenergic receptor (AR) undergoes rapid agonist-promoted desensitization due
to phosphorylation by G protein-coupled receptor kinases (GRKs) 2 and 3 at serines in the
third intracellular loop of the receptor. In contrast, the α 2C AR fails to display such
desensitization or phosphorylation, which has been presumed to be due to this receptor
lacking GRK phosphorylation sites. However, the α 2C AR has multiple serines and
threonines in putative favorable motifs within its third intracellular loop. We considered that …