Single-Molecule Imaging Reveals Differential AT1R Stoichiometry Change in Biased Signaling.

ABSTRACT: G protein-coupled receptors (GPCRs) represent promising therapeutic targets due to their involvement in numerous physiological processes mediated by downstream G protein- and β-arrestin-mediated signal transduction cascades. Although the precise control of GPCR signaling pathways is therapeutically valuable, the molecular details for governing biased GPCR signaling remain elusive. The Angiotensin II type 1 receptor (AT1R), a prototypical class A GPCR with profound implications for cardiovascular functions, has become a focal point for biased ligand-based clinical interventions. Herein, we used single-molecule live-cell imaging techniques to evaluate the changes in stoichiometry and dynamics of AT1R with distinct biased ligand stimulations in real time. It was revealed that AT1R existed pre

SUBMITTER: Qin G 

PROVIDER: S-EPMC10778740 | biostudies-literature | 2023 Dec

REPOSITORIES: biostudies-literature