ArticleNaunyn-Schmiedeberg's archives of pharmacology2000
Activation of the A3 adenosine receptor affects cell cycle progression and cell growth.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 88 citations in OpenAlex.
- Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual AJournal of medicinal chemistry · 2023Article
- Systematic Design of Adenosine Analogs as Inhibitors of aJournal of medicinal chemistry · 2023Article
- Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human AMedChemComm · 2018Article
- Mitochondrial and caspase pathways are involved in the induction of apoptosis by IB-MECA in ovarian cancer cell lines.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2014Article
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- Antiproliferative effects of selective adenosine receptor agonists and antagonists on human lymphocytes: evidence for receptor-independent mechanisms.Purinergic signalling · 2013Article
- Effects of synthetic A3 adenosine receptor agonists on cell proliferation and viability are receptor independent at micromolar concentrations.Journal of physiology and biochemistry · 2013Article
- Involvement of ecto-5'-nucleotidase/CD73 in U138MG glioma cell adhesion.Molecular and cellular biochemistry · 2012Article
- Activation of A1, A2A, or A3 adenosine receptors attenuates lung ischemia-reperfusion injury.The Journal of thoracic and cardiovascular surgery · 2010Article
- The Anti-Cancer Effect of AImmunology, endocrine & metabolic agents in medicinal chemistry · 2007Article
- 2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.Journal of medicinal chemistry · 2006Article
- Molecular modelling study of 2-phenylethynyladenosine (PEAdo) derivatives as highly selective A₃ adenosine receptor ligands.Purinergic signalling · 2006Article
- Modulation of the Akt/Ras/Raf/MEK/ERK pathway by A₃ adenosine receptor.Purinergic signalling · 2006Article
- Synthesis of hypermodified adenosine derivatives as selective adenosine A3 receptor ligands.Bioorganic & medicinal chemistry · 2006Article
- Progress in the pursuit of therapeutic adenosine receptor antagonists.Medicinal research reviews · 2006Review
- Exploring human adenosine A3 receptor complementarity and activity for adenosine analogues modified in the ribose and purine moiety.Bioorganic & medicinal chemistry · 2005Article
- A3 adenosine receptors in human astrocytoma cells: agonist-mediated desensitization, internalization, and down-regulation.Molecular pharmacology · 2002Article
- Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist.Journal of medicinal chemistry · 2002Article
- p53-Independent induction of Fas and apoptosis in leukemic cells by an adenosine derivative, Cl-IB-MECA.Biochemical pharmacology · 2002Article
- Pharmacological and biochemical characterization of adenosine receptors in the human malignant melanoma A375 cell line.British journal of pharmacology · 2001Article
Corrections and comments
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Authors and funding
10 authors at 5 institutions in 3 countries.
Funding
Abstract
The A3 adenosine receptor has been implicated in modulation of cell growth. As a first step to the characterization of the underlying mechanisms, we exposed Chinese hamster ovary (CHO) cells transfected with the human A3 receptor (A3R-CHO) to selective A3 receptor ligands. At micromolar concentrations, the A3 agonists N6-(3-iodobenzyl)-adenosine-5'-N-methyluronamide (IB-MECA) and its 2-chloro derivative Cl-IB-MECA reduced cell number, with no effects on either parental CHO cells (not expressing any adenosine receptor), or CHO cells transfected with the human A1 receptor. Cl-IB-MECA also reduced cell number in the human HEK293 cell line transfected with the human A3 receptor cDNA as opposed to the respective untransfected wild-type cells. In A3R-CHO, agonist-induced effects were antagonized by nanomolar concentrations of A3 antagonists, including the triazoloquinazoline derivative MRS 1220, the dihydropyridine derivative MRS 1191, and the triazolonaphthyridine derivative L-249,313. A3 agonist-induced effects were not due to modulation of cell adhesion, nor to necrosis or apoptosis. Growth curves revealed highly impeded growth, and flow-cytometric analysis showed markedly reduced bromodeoxyuridine incorporation into nuclei. The effect on cell cycle was completely antagonized by MRS1191. Hence, activation of the human A3 receptor in A3R-CHO results in markedly impaired cell cycle progression, suggesting an important role for this adenosine receptor subtype in cell cycle regulation and cell growth.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.