Why Are A2B Receptors Low-Affinity Adenosine Receptors? Mutation of Asn273 to Tyr Increases Affinity of Human A2B Receptor for 2-(1-Hexynyl)adenosine

2000 ◽  
Vol 58 (6) ◽  
pp. 1349-1356 ◽  
Author(s):  
Margot W. Beukers ◽  
Hans den Dulk ◽  
Erica W. van Tilburg ◽  
Jaap Brouwer ◽  
Adriaan P. Ijzerman
Keyword(s):  
Adenosine Receptors ◽  
A2b Receptor

Canine Mast Cell Adenosine Receptors: Cloning and Expression of the A3 Receptor and Evidence that Degranulation Is Mediated by the A2B Receptor

1997 ◽  
Vol 52 (5) ◽  
pp. 846-860 ◽  
Author(s):  
John A. Auchampach ◽  
Xiaowei Jin ◽  
Tina C. Wan ◽  
George H. Caughey ◽  
Joel Linden
Keyword(s):  
Mast Cell ◽  
Adenosine Receptors ◽  
Cloning And Expression ◽  
A2b Receptor

scholarly journals Adenosine receptors in regulation of dendritic cell differentiation and function

Blood ◽  
2008 ◽  
Vol 112 (5) ◽  
pp. 1822-1831 ◽  
Author(s):  
Sergey V. Novitskiy ◽  
Sergey Ryzhov ◽  
Rinat Zaynagetdinov ◽  
Anna E. Goldstein ◽  
Yuhui Huang ◽  
...  
Keyword(s):  
Adenosine Receptors ◽  
Peritoneal Macrophages ◽  
Extracellular Adenosine ◽  
Dendritic Cell Differentiation ◽  
Distinct Cell ◽  
A2b Receptor ◽  
And Function ◽  
Knockout Animals ◽  
Mouse Peritoneal Macrophages

Abstract Differentiation of functional dendritic cells (DCs) critically depends on the microenvironment. DCs differentiate in hypoxic tumor sites and inflamed or damaged tissue. Because local concentrations of adenosine reach high physiologically relevant levels in these conditions, we assessed the expression of adenosine receptors and the effect of their activation on differentiation of human monocytes and mouse peritoneal macrophages and hematopoietic progenitor cells (HPCs) into myeloid DCs. Stimulation of adenosine receptors skews DC differentiation toward a distinct cell population characterized by expression of both DC and monocyte/macrophage cell surface markers. Pharmacologic analysis and experiments with cells from A2B adenosine receptor knockout mice identified A2B receptor as the mediator of adenosine effects on DCs. Unlike normal myeloid DCs, adenosine-differentiated DCs have impaired allostimulatory activity and express high levels of angiogenic, pro-inflammatory, immune suppressor, and tolerogenic factors, including VEGF, IL-8, IL-6, IL-10, COX-2, TGF-β, and IDO. They promoted tumor growth if injected into tumors implanted in mice. Using adenosine desaminase knockout animals, we showed that DCs with proangiogenic phenotype are highly abundant under conditions associated with elevated levels of extracellular adenosine in vivo. Adenosine signaling through A2B receptor is an important factor of aberrant DC differentiation and generation of tolerogenic, angiogenic, and proinflammatory cells.

280-LB: Role of A1 and A3 Adenosine Receptors in Whole Body Glucose Metabolism

Diabetes ◽  
2019 ◽  
Vol 68 (Supplement 1) ◽  
pp. 280-LB ◽  
Author(s):  
SHANU JAIN ◽  
DILIP K. TOSH ◽  
MARC REITMAN ◽  
KENNETH A. JACOBSON
Keyword(s):  
Glucose Metabolism ◽  
Adenosine Receptors ◽  
Whole Body

PET Imaging of Adenosine Receptors in Diseases

2019 ◽  
Vol 19 (16) ◽  
pp. 1445-1463 ◽  
Author(s):  
Jindian Li ◽  
Xingfang Hong ◽  
Guoquan Li ◽  
Peter S. Conti ◽  
Xianzhong Zhang ◽  
...  
Keyword(s):  
Pet Imaging ◽  
Adenosine Receptors ◽  
Neurological Diseases ◽  
G Protein Coupled Receptors ◽  
Extracellular Adenosine ◽  
Positron Emission ◽  
Imaging Probes ◽  
Pet Probes ◽  
Cancer And Inflammation ◽  
G Protein Coupled

Adenosine receptors (ARs) are a class of purinergic G-protein-coupled receptors (GPCRs). Extracellular adenosine is a pivotal regulation molecule that adjusts physiological function through the interaction with four ARs: A1R, A2AR, A2BR, and A3R. Alterations of ARs function and expression have been studied in neurological diseases (epilepsy, Alzheimer’s disease, and Parkinson’s disease), cardiovascular diseases, cancer, and inflammation and autoimmune diseases. A series of Positron Emission Tomography (PET) probes for imaging ARs have been developed. The PET imaging probes have provided valuable information for diagnosis and therapy of diseases related to alterations of ARs expression. This review presents a concise overview of various ARs-targeted radioligands for PET imaging in diseases. The most recent advances in PET imaging studies by using ARs-targeted probes are briefly summarized.

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