title: Investigational A₃ adenosine receptor targeting agents.
abstract: BACKGROUND
  Adenosine is an endogenous nucleoside that accumulates in the extracellular space in response to metabolic stress and cell damage. Extracellular adenosine is a signaling molecule that signals by activating four GPCRs: the A(1), A(2A), A(2B) and A(3) receptors. Since the discovery of A(3) adenosine receptors, accumulating evidence has identified these receptors as potential targets for therapeutic intervention.
  
  
  METHODS
  A(3) adenosine receptors are expressed on the surface of most immune cell types, including neutrophils, macrophages, dendritic cells, lymphocytes and mast cells. A(3) adenosine receptor activation on immune cells governs a broad array of immune cell functions, which include cytokine production, degranulation, chemotaxis, cytotoxicity, apoptosis and proliferation. In accordance with their multitudinous immunoregulatory actions, targeting A(3) adenosine receptors has been shown to impact the course of a wide spectrum of immune-related diseases, such as asthma, rheumatoid arthritis, cancer, ischemia and inflammatory disorders.
  
  
  CONCLUSIONS
  Given the existence of both preclinical and early clinical data supporting the utility of A(3) adenosine receptor ligands in treating immune-related diseases, further development of A(3) adenosine receptor ligands is anticipated.
authors: University of Medicine and Dentistry of New Jersey, New Jersey Medical School, Department of Surgery, 185 South Orange Avenue, Newark, NJ 07103, USA.
authors: Balázs
authors: B
authors: Koscsó
authors: Balázs
authors: B
authors: Csóka
authors: Pál
authors: P
authors: Pacher
authors: György
authors: G
authors: Haskó
mesh_terms: D058909:Adenosine A3 Receptor Agonists / Q000494:pharmacology*; D058918:Adenosine A3 Receptor Antagonists / Q000494:pharmacology*; D000818:Animals; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D007154:Immune System Diseases / Q000188:drug therapy / Q000503:physiopathology; D008024:Ligands; D043684:Receptor, Adenosine A3 / Q000187:drug effects* / Q000276:immunology / Q000378:metabolism
chemical_list: D058909:Adenosine A3 Receptor Agonists; D058918:Adenosine A3 Receptor Antagonists; D008024:Ligands; D043684:Receptor, Adenosine A3