Corpus ID: 12871161

Brand „ Agonist-induced Signaling and Endocytosis of the Adenosine A 2 A Receptor “

  title={Brand „ Agonist-induced Signaling and Endocytosis of the Adenosine A 2 A Receptor “},
  author={Frank Brand and Gunnar Schulte},
Cover (and back side), Alexa488-APEC staining (green) of the adenosine A 2A receptor in living Chinese hamster ovary cell transiently transfected with pcDNA3 A 2A R as well as pAS β-arrestin2-RFP (red). 


Desensitization of the canine A2a adenosine receptor: delineation of multiple processes.
Data suggest that A2aAR desensitization is mediated by multiple, temporally distinct, agonist-dependent processes, whereas long term down- regulation of receptor number and up-regulation of inhibitory G proteins mediate long term adaptation. Expand
beta-Arrestin 1 and 2 differentially regulate heptahelical receptor signaling and trafficking.
Results suggest that sequestration of various heptahelical receptors is regulated differently by the two beta-arrestins, whereas both isoforms are capable of supporting receptor desensitization and down-regulation. Expand
The G(s)-coupled adenosine A(2B) receptor recruits divergent pathways to regulate ERK1/2 and p38.
Adenosine A(2B) receptors have been suggested to influence cell differentiation and proliferation. Human adenosine A(2B) receptors expressed in Chinese hamster ovary cells mediate phosphorylation andExpand
Adenosine A3 receptors: novel ligands and paradoxical effects.
  • K. Jacobson
  • Medicine, Chemistry
  • Trends in pharmacological sciences
  • 1998
How A3 receptor agonists might be useful in treating inflammatory conditions, possibly through their inhibition of tumour necrosis factor alpha (TNF-alpha) release, which has been shown in macrophages is described. Expand
Inhibition of NMDA receptor-mediated currents in isolated rat hippocampal neurones by adenosine A1 receptor activation
The effect of the stable adenosine analogue, 2-chloroadenosine (CADO), on the currents elicited by iontophoretic application of N-methyl-d-aspartate (NMDA) to pyramidal cells acutely dissociated fromExpand
Identification of an A2a adenosine receptor domain specifically responsible for mediating short-term desensitization.
The data suggest that while the majority of the A2aAR carboxyl-terminus is dispensable with regard to observing functional desensitization, the integrity of Thr 298 is essential for observing agonist-stimulated receptor phosphorylation and short-term desensITization but not long-term Desensitized function. Expand
The sustainability of interactions between the orexin-1 receptor and beta-arrestin-2 is defined by a single C-terminal cluster of hydroxy amino acids and modulates the kinetics of ERK MAPK regulation.
It is indicated that a single cluster of hydroxy amino acids within the C-terminal seven amino acids of the orexin-1 receptor determine the sustainability of interaction with beta-arrestin-2, and an important role of beta-Arrestin scaffolding in defining the kinetics of orexIn-1 receptors-mediated ERK MAPK activation is indicated. Expand
New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells.
A series of red-emitting agonists for the human adenosine A1-receptor are developed that retain potent and efficacious agonist activity, and their suitability for use in FCS was demonstrated by quantification of agonist binding in small areas of cell membrane. Expand
Tumor necrosis factor-alpha prevents desensitization of Galphas-coupled receptors by regulating GRK2 association with the plasma membrane.
A novel form of cross-talk between TNF-alpha receptors and GPCR function is suggested by preventing agonist-induced desensitization of GPCRs by diminishing agonists-dependent recruitment of GRK2 and beta-arrestin to PM by a SMase pathway-mediated mechanism. Expand
Adenosine, an endogenous distress signal, modulates tissue damage and repair
  • B. Fredholm
  • Biology, Medicine
  • Cell Death and Differentiation
  • 2007
It is argued that drugs targeting adenosine receptors might be useful adjuncts in many therapeutic approaches, usually having a cytoprotective function. Expand