ArticleBiochemical pharmacology2008
The A3 adenosine receptor agonist CF502 inhibits the PI3K, PKB/Akt and NF-kappaB signaling pathway in synoviocytes from rheumatoid arthritis patients and in adjuvant-induced arthritis rats.
Article in Biochemical pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers, 1 of them a synthesis that pooled it.
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Who cites it
33 citing papers in PubMed, 1 synthesis or guideline pooled it, 69 citations in OpenAlex.
- Efficacy and safety of Piclidenoson in the treatment of plaque psoriasis: a systematic review and meta-analysis of randomized controlled trials.Archives of dermatological research · 2024Pooled it
- Genetic and functional modulation by agonist MRS5698 and allosteric enhancer LUF6000 at the native APurinergic signalling · 2024Article
- Istradefylline modulates purinergic enzymes and reduces malignancy-associated factors in B16F10 melanoma cells.Purinergic signalling · 2023Article
- Pharmacology of Adenosine Receptors: Recent Advancements.Biomolecules · 2023Review
- Prolonged administration of total glucosides of paeony improves intestinal immune imbalance and epithelial barrier damage in collagen-induced arthritis rats based on metabolomics-network pharmacology integrated analysis.Frontiers in pharmacology · 2023Article
- Adenosine receptors as emerging therapeutic targets for diabetic kidney disease.Kidney research and clinical practice · 2022Article
- Drugs Targeting the A3 Adenosine Receptor: Human Clinical Study Data.Molecules (Basel, Switzerland) · 2022Review
- Diagnostic and therapeutic strategies for non-alcoholic fatty liver disease.Frontiers in pharmacology · 2022Review
- Anti-Inflammatory Effects of Endogenously Released Adenosine in Synovial Cells of Osteoarthritis and Rheumatoid Arthritis Patients.International journal of molecular sciences · 2021Article
- Adenosine and Inflammation: Here, There and Everywhere.International journal of molecular sciences · 2021Review
- Adenosine AJournal of neuroinflammation · 2020Article
- Activation of Adenosine AInternational journal of molecular sciences · 2020Article
- The A3 adenosine receptor agonist, namodenoson, ameliorates non‑alcoholic steatohepatitis in mice.International journal of molecular medicine · 2019Article
- The Purinergic System as a Pharmacological Target for the Treatment of Immune-Mediated Inflammatory Diseases.Pharmacological reviews · 2019Review
- Dysregulation of Adenosinergic Signaling in Systemic and Organ-Specific Autoimmunity.International journal of molecular sciences · 2019Review
- Targeting the ADrug design, development and therapy · 2019Review
- AMedicinal research reviews · 2018Review
- Inhibition of IL-17 and IL-23 in Human Keratinocytes by the AJournal of immunology research · 2018Article
- Role and Function of AInternational journal of molecular sciences · 2017Article
- An adenosine A3 receptor agonist inhibits DSS-induced colitis in mice through modulation of the NF-κB signaling pathway.Scientific reports · 2015Article
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Authors and funding
12 authors at 5 institutions in 2 countries.
Funding
Abstract
The A(3) adenosine receptor (A(3)AR) is over-expressed in inflammatory cells and was defined as a target to combat inflammation. Synthetic agonists to this receptor, such as IB-MECA and Cl-IB-MECA, exert an anti-inflammatory effect in experimental animal models of adjuvant- and collagen-induced arthritis. In this study we present a novel A(3)AR agonist, CF502, with high affinity and selectivity at the human A(3)AR. CF502 induced a dose dependent inhibitory effect on the proliferation of fibroblast-like synoviocytes (FLS) via de-regulation of the nuclear factor-kappa B (NF-kappaB) signaling pathway. Furthermore, CF502 markedly suppressed the clinical and pathological manifestations of adjuvant-induced arthritis (AIA) in a rat experimental model when given orally at a low dose (100 microg/kg). As is typical of other G-protein coupled receptors, the A(3)AR expression level was down-regulated shortly after treatment with agonist CF502 in paw and in peripheral blood mononuclear cells (PBMCs) derived from treated AIA animals. Subsequently, a decrease in the expression levels of protein kinase B/Akt (PKB/Akt), IkappaB kinase (IKK), I kappa B (IkappaB), NF-kappaB and tumor necrosis factor-alpha (TNF-alpha) took place. In addition, the expression levels of glycogen synthase kinase-3 beta (GSK-3beta), beta-catenin, and poly(ADP-ribose)polymerase (PARP), known to control the level and activity of NF-kappaB, were down-regulated upon treatment with CF502. Taken together, CF502 inhibits FLS growth and the inflammatory manifestations of arthritis, supporting the development of A(3)AR agonists for the treatment of rheumatoid arthritis.
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