β-Arrestins Regulate Protease-activated Receptor-1 Desensitization but Not Internalization or Down-regulation

C-terminal fusion of eGFP to the bradykinin B2 receptor strongly affects down-regulation but not receptor internalization or signaling.

A functional comparison was made between the wild-type bradykinin B2 receptor (B2wt) and the chimera B2eGFP (enhanced green-fluorescent protein fused to the C-terminus of B2wt), both stably expressed in HEK 293 cells. There was almost no difference in terms of ligand-inducible receptor phosphorylation and internalization, signal transduction (accumulation of inositol phosphates) or expression a...

Thrombin-Induced Calpain Activation Promotes Protease-Activated Receptor 1 Internalization

The serine protease thrombin activates Protease-Activated Receptors (PARs), a family of G-protein-coupled receptors (GPCRs) activated by the proteolytic cleavage of their extracellular N-terminal domain. Four members of this family have been identified: PAR1-4. The activation of Protease-Activated Receptor 1(PAR1), the prototype of this receptor family, leads to an increase in intracellular Ca+...

Agonist-induced internalization of leukotriene B(4) receptor 1 requires G-protein-coupled receptor kinase 2 but not arrestins.

The leukotriene B(4) (LTB(4)) receptor (BLT1) becomes desensitized upon repeated agonist stimulation. Little is known, however, about BLT1 internalization, which follows desensitization in most G-protein-coupled receptors (GPCR). In the current study, transiently expressed BLT1 readily internalized, after LTB(4) stimulation, in RBL-2H3 cells that express high levels of endogenous GPCR kinase 2 ...

Clathrin-dependent Internalization of Protease-activated Receptor-1: Regulation by Ubiquitination and Epsin

Breann Louise Wolfe Clathrin-dependent Internalization of Protease-activated Receptor-1: Regulation by Ubiquitination and Epsin (Under the direction of Dr. JoAnn Trejo) Thrombin, the main effector protease of the coagulation cascade elicits its cellular effects via activation of a family of G-protein coupled receptors (GPCRs) called proteaseactivated receptors (PARs). PAR1, the prototype of thi...

1 Down - regulation of Protease - activated Receptor - 1 Is Regulated by Sorting