5 documents found

Helix-bundle and C-terminal GPCR domains differentially influence GRK-specific functions and β-arrestin-mediated regulation

G protein-coupled receptors (GPCRs) orchestrate diverse physiological responses via signaling through G proteins, GPCR kinases (GRKs), and arrestins. While most G protein functions are well-established, the contributions of GRKs and arrestins remain incompletely understood. Here, we investigate the influence…
[London]: Springer Nature, 2025-07-01

β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the same GPCR in living cells

Abstract β-arrestins mediate regulatory processes for over 800 different G protein-coupled receptors (GPCRs) by adopting specific conformations that result from the geometry of the GPCR–β-arrestin complex. However, whether β-arrestin1 and 2 respond differently for binding to the same GPCR is still unknown.…
[London]: Springer Nature, 2022-09-26

GPCR kinase knockout cells reveal the impact of individual GRKs on arrestin binding and GPCR regulation

G protein-coupled receptors (GPCRs) activate G proteins and undergo a complex regulation by interaction with GPCR kinases (GRKs) and the formation of receptor–arrestin complexes. However, the impact of individual GRKs on arrestin binding is not clear. We report the creation of eleven combinatorial HEK293…
[London]: Springer Nature, 2022-01-27

Differential analysis of GPCR-induced dynamic conformational change in β-arrestin1 and 2

G protein-coupled receptors (GPCRs) constitute the largest family of membrane receptors in human physiology, comprising more than 800 different genes. They sense diverse extracellular signals and initiate intracellular signaling responses via the activation of specific G proteins. The downregulation…

Differential regulation of GPCRs : Are GRK expression levels the key?

G protein-coupled receptors (GPCRs) comprise the largest family of transmembrane receptors and their signal transduction is tightly regulated by GPCR kinases (GRKs) and β-arrestins. In this review, we discuss novel aspects of the regulatory GRK/β-arrestin system. Therefore, we briefly revise the origin…
Lusanne: Frontiers Media S.A., 2021-05-24