We conducted the present study to investigate protein expression and functioning of A2A and A2B adenosine receptors (ARs) in neutrophils of patients affected by systemic sclerosis (SSc). The presence of A2A and A2B ARs was assessed by immunoblotting using specific antibodies. Equilibrium A2A and A2B ARs binding parameters were evaluated by radioligand binding assay. Functional studies were conducted to investigate coupling of the A2B AR to the adenylyl cyclase pathway. This is the first report of the use of Western blot analysis to confirm the presence of A2A and A2B ARs in human neutrophils. No significant changes in A2A AR binding parameters or expression levels were detected between SSc patients and healthy control individuals. A significant decrease (65%) in the maximum density of A2B AR binding sites occurred in SSc neutrophils, whereas no changes in the affinity constant values were found. Moreover, a decrease in A2B AR mediated adenylyl cyclase activity was observed in patients with SSc. Our findings demonstrate the occurrence of selective alterations in A2B AR density and signalling in SSc.
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http://dx.doi.org/10.1186/ar1468 | DOI Listing |
Mol Divers
January 2025
Chemometrics and Cheminformatics Laboratory, Department of Analytical Chemistry, Tarbiat Modares University, Tehran, Iran.
Adenosine receptors (A, A, A, A) play critical roles in cellular signaling and are implicated in various physiological and pathological processes, including inflammations and cancer. The main aim of this research was to investigate structure-activity relationships (SAR) to derive models that describe the selectivity and activity of inhibitors targeting Adenosine receptors. Structural information for 16,312 inhibitors was collected from BindingDB and analyzed using machine learning methods.
View Article and Find Full Text PDFCirc Rep
January 2025
Department of Diabetes/Endocrinology and Metabolism, Minoh City Hospital Osaka Japan.
Background: The urinary albumin-to-creatinine ratio (UACR) or urinary protein-to-creatinine ratio (UPCR) has been reported as predictors of cardiovascular and renal events. We aimed to evaluate the impact of changes in proteinuria severity on the prognosis of hypertensive patients post-esaxerenone initiation.
Methods And Results: Hypertensive patients who commenced esaxerenone (n=164) were classified into 3 groups according to baseline UACR or UPCR, based on the modified proteinuria severity classification: A1 (normal; n=35); A2 (microalbuminuria/mild proteinuria; n=49); and A3 (macroalbuminuria/severe proteinuria; n=80).
Int J Mol Sci
December 2024
Atherothrombosis Research Centre/Laboratory of Biochemistry, Department of Chemistry, University of Ioannina, 451 10 Ioannina, Greece.
Ticagrelor, a reversible platelet P2Y receptor antagonist, exerts various pleiotropic actions, some of which are at least partially mediated through adenosine. We studied the ticagrelor and adenosine effect on the angiogenic properties of progenitor CD34-derived endothelial colony-forming cells (ECFCs). Angiogenesis studies were performed in vitro using capillary-like tube formation and spheroid-based angiogenesis assays.
View Article and Find Full Text PDFAndrology
December 2024
Faculty of Medicine, Department of Obstetrics, Gynecology and Reproduction, Centre Hospitalier Universitaire de Québec - Research Centre, and Centre de Recherche en Reproduction, Développement et Santé Intergénérationnelle - Université Laval, Québec, QC, Canada.
Introduction: The epididymis creates an optimal acidic luminal environment for sperm maturation and storage. In epididymal principal cells (PCs), proton secretion is activated by the accumulation of the sodium-proton exchanger type 3, NHE3 (SLC9A3), in apical stereocilia. PCs also secrete ATP, which is hydrolyzed into adenosine by ectonucleotidases.
View Article and Find Full Text PDFCancer Biol Med
December 2024
Biotherapy Center and Cancer Center, the First Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China.
This review examined the critical role of adenosine signaling in modulating the behavior of tumor-associated macrophages (TAMs), a key determinant of the tumor microenvironment (TME). Adenosine is an immunosuppressive metabolite that is highly enriched in the TME due to elevated expression of adenosine triphosphatase (ATPase). Adenosine influences polarization of TAMs through A2A and A2B receptors, which drives a phenotype that supports tumor progression and immune evasion.
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