... are supported by G-protein-independent, β-arrestin-dependent signalling events. In the present article, we review current knowledge on structural and signalling properties of ACRs that are changing our view on this entire class of receptors from silent to endogenous β-arrestin-biased signalling receptors...

..., kinases and β-arrestins) and on the dynamics of the interconversion among all these states. To improve on this will require collaborations between biophysicists and molecular modellers, as well as biochemists and pharmacologists, to use existing techniques and develop new tools to solve the problems...

... in catalytic function, each isoform appears to serve a non-superfluous regulatory role. For example, a β-arrestin-sequestered subpopulation of the PDE4D5 isoform specifically regulates the phosphorylation of the β 2 -AR (β 2 -adrenergic receptor) by PKA (protein kinase A; also called cAMP-dependent protein...

...K.D.G. Pfleger; M.B. Dalrymple; J.R. Dromey; K.A. Eidne β-Arrestins 1 and 2 are ubiquitously expressed intracellular adaptor and scaffolding proteins that play important roles in GPCR (G-protein-coupled receptor) desensitization, internalization, intracellular trafficking and G-protein-independent...

..., by using either a selective inhibitor or siRNA knockout, results in accelerated isoprenaline-induced GRK2 recruitment, GRK2 phosphorylation of the β 2 Ar and β-arrestin translocation to the β 2 Ar. Surprisingly, however, we have also shown that these effects can occur, albeit to a reduced extent, merely...

... isoform preferentially interacts with the signalling scaffold protein β-arrestin and is thereby recruited to the β 2 -AR upon agonist challenge. Delivery of an active PDE to the site of cAMP synthesis at the plasma membrane specifically attenuates the activity of a pool of PKA (protein kinase...

... is attenuated by β-arrestin-mediated desensitization and endocytosis, and by lysosomal targeting and degradation, which requires ubiquitination of PAR 2 . β-Arrestins also act as scaffolds for the assembly of multi-protein signalling complexes that determine the location and function of activated mitogen...

... acetylcholine receptors (mAChRs). Using the transient expression system of HEK-293 cells, we showed that the M 1 , M 3 and M 4 mAChRs are internalized into clathrin-coated vesicles and recycle back to the plasma membrane. This internalization pathway is dependent on the concerted action of β-arrestin, c-Src...