Fusion of the β₂-adrenergic receptor with either Gαs or βarrestin-2 produces constitutive signaling by each pathway and induces gain-of-function in BEAS-2B cells.

ABSTRACT: The β₂AR is a prototypical G protein-coupled receptor (GPCR) known to orchestrate different cellular responses by the stimulation of specific signaling pathways. The best-established signaling pathways for the β₂AR are the canonical Gs pathway and the alternative β arrestin 2 (βarr2) pathway. Exploring each pathway separately remains a challenging task due to the dynamic nature of the receptor. Here, we fused the β₂AR with its cognate transducers, Gαs and βarr2, using short linkers as a novel approach for restricting the conformation of the receptor and preferentially activating one of its two signaling pathways. We characterized the behavior of our fusion proteins β₂AR-Gαs and β₂AR-βarr2 in HEK293 cells by measuring their constitutive

SUBMITTER: Lucero-Garcia Rojas EY 

PROVIDER: S-EPMC9721090 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature