Results 31 to 40 of about 2,574,999 (363)
Allosteric modulation of adenosine receptors [PDF]
Purinergic Signalling, 2008 Allosteric ligands for G protein-coupled receptors (GPCRs) may alter receptor conformations induced by an orthosteric ligand. These modulators can thus fine-tune classical pharmacological responses. In this review we will describe efforts to synthesize and characterize allosteric modulators for one particular GPCR subfamily, the adenosine receptors ...
Anikó Göblyös, Ad P. IJzerman
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Internalization and desensitization of adenosine receptors [PDF]
Purinergic Signalling, 2007 Until now, more than 800 distinct G protein-coupled receptors (GPCRs) have been identified in the human genome. The four subtypes of the adenosine receptor (A(1), A(2A), A(2B) and A(3) receptor) belong to this large family of GPCRs that represent the most widely targeted pharmacological protein class. Since adenosine receptors are widespread throughout
Klaasse, E.C. +3 more
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Low expression of CD39 and CD73 genes in centenarians compared with octogenarians
Immunity & Ageing, 2017 Ageing involves a progressive decline of the body’s regulatory systems including immune system. Adenosine regulates immune function by interaction with its receptors, mainly adenosine A2A receptor, present on the surface of immune cells.
Almudena Crooke +5 more
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Adenosine A2A Receptor Blockade as an Immunotherapy for Treatment-Refractory Renal Cell Cancer.
Cancer Discovery, 2019 Adenosine mediates immunosuppression within the tumor microenvironment through triggering adenosine 2A receptors (A2AR) on immune cells. To determine whether this pathway could be targeted as an immunotherapy, we performed a phase 1 clinical trial with a
L. Fong +32 more
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Adenosine Receptors and the Kidney [PDF]
, 2009 The autacoid, adenosine, is present in the normoxic kidney and generated in the cytosol as well as at extracellular sites. The rate of adenosine formation is enhanced when the rate of ATP hydrolysis prevails over the rate of ATP synthesis during increased tubular transport work or during oxygen deficiency.
Volker Vallon, Hartmut Osswald
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Fluorescent ligands for adenosine receptors [PDF]
Bioorganic & Medicinal Chemistry Letters, 2013 Interest is increasing in developing fluorescent ligands for characterization of adenosine receptors (ARs), which hold a promise of usefulness in the drug discovery process. The size of a strategically labeled AR ligand can be greatly increased after the attachment of a fluorophore. The choice of dye moiety (e.g.
Eszter Kozma +7 more
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Intracellular ATP concentration contributes to the cytotoxic and cytoprotective effects of adenosine. [PDF]
PLoS ONE, 2013 Extracellular adenosine (ADE) interacts with cells by two pathways: by activating cell surface receptors at nanomolar/micromolar concentrations; and by interfering with the homeostasis of the intracellular nucleotide pool at millimolar concentrations ...
Shujue Li +8 more
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Chemical Probes for the Adenosine Receptors [PDF]
Pharmaceuticals, 2019 Research on the adenosine receptors has been supported by the continuous discovery of new chemical probes characterized by more and more affinity and selectivity for the single adenosine receptor subtypes (A1, A2A, A2B and A3 adenosine receptors). Furthermore, the development of new techniques for the detection of G protein-coupled receptors (GPCR ...
Federico S., Lassiani L., Spalluto G.
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Adenosine-Metabolizing Enzymes, Adenosine Kinase and Adenosine Deaminase, in Cancer
Biomolecules, 2022 The immunosuppressive effect of adenosine in the microenvironment of a tumor is well established. Presently, researchers are developing approaches in immune therapy that target inhibition of adenosine or its signaling such as CD39 or CD73 inhibiting ...
Galina Zhulai +3 more
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Structure of the adenosine A2A receptor bound to an engineered G protein
Nature, 2016 G-protein-coupled receptors (GPCRs) are essential components of the signalling network throughout the body. To understand the molecular mechanism of G-protein-mediated signalling, solved structures of receptors in inactive conformations and in the active
B. Carpenter +4 more
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