Uncovering conserved networks and global conformational changes in G protein-coupled receptor kinases.

ABSTRACT: G protein-coupled receptor kinases (GRKs) are essential regulators of signaling pathways mediated by G protein-coupled receptors. Recent research suggests that GRK-mediated phosphorylation patterns dictate functional selectivity, leading to biased cellular responses. However, a comprehensive understanding of the structural mechanisms at the single-residue level remains elusive. This study aims to define the general conformational dynamics of GRKs with a particular focus on quantifying the transitions between the closed and open states. Specifically, we examined these transitions, classified based on the ionic lock between the regulatory G protein signaling homology domain and kinase domain. To facilitate a precise structural comparison, we assigned common labels to topologically identical

SUBMITTER: Seo MJ 

PROVIDER: S-EPMC11472376 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature