... infections by curbing the responsiveness of these cells to inflammatory and infectious stimuli. Mechanistically, Norbin regulates cell responses through binding to its interactors, in particular to a wide range of G protein-coupled receptors (GPCRs). Norbin association with GPCRs controls GPCR trafficking...

...Gert N. Moll; Anneke Kuipers; Rick Rink; Tjibbe Bosma; Louwe de Vries; Pawel Namsolleck The conformation with which natural agonistic peptides interact with G protein-coupled receptor(s) (GPCR(s)) partly results from intramolecular interactions such as hydrogen bridges or is induced by ligand...

... with the endogenous agonist noradrenaline are highlighted in blue, the oxymethylene linker that is conserved among antagonists is highlighted in red. Head groups are the substituents at the right hand of the ligand; tail regions are to the left of the secondary amine group. activation agonist GPCR helix 5...

...Eamonn Kelly Ligand bias refers to the ability of a drug at a receptor to activate selectively particular cell signalling pathways over others, in a way that cannot be explained by traditional models of receptor theory. For a physiologically and therapeutically important GPCR (G-protein-coupled...

..., is associated with low activity of the PKA pathway. We have studied how different nutrients trigger rapid activation of the pathway. Glucose and sucrose activate cAMP synthesis through a G-protein-coupled receptor system, consisting of the GPCR Gpr1, the Gα protein Gpa2 and its RGS protein Rgs2. Glucose is also...

...M. von Zastrow Many G-protein-coupled receptors (GPCRs) undergo agonist-induced endocytosis. Endocytosis contributes to distinct processes that regulate the number and functional activity of receptors present in the plasma membrane, contributing to the well described processes of receptor...