Autoregulation of GPCR signalling through the third intracellular loop.

ABSTRACT: The third intracellular loop (ICL3) of the G protein-coupled receptor (GPCR) fold is important for the signal transduction process downstream of receptor activation^1-3. Despite this, the lack of a defined structure of ICL3, combined with its high sequence divergence among GPCRs, complicates characterization of its involvement in receptor signalling⁴. Previous studies focusing on the β₂ adrenergic receptor (β₂AR) suggest that ICL3 is involved in the structural process of receptor activation and signalling^5-7. Here we derive mechanistic insights into the role of ICL3 in β₂AR signalling, observing that ICL3 autoregulates receptor activity through a dynamic conformational equilibrium between states that block or expose the recep

SUBMITTER: Sadler F 

PROVIDER: S-EPMC10033409 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature