ArticleThe Journal of pharmacology and experimental therapeutics2011
{Beta}2-adrenergic receptor agonists inhibit the proliferation of 1321N1 astrocytoma cells.
Article in The Journal of pharmacology and experimental therapeutics, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 39 citations in OpenAlex.
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- β adrenergic receptor modulated signaling in glioma models: promoting β adrenergic receptor-β arrestin scaffold-mediated activation of extracellular-regulated kinase 1/2 may prove to be a panacea in the treatment of intracranial and spinal malignancy and extra-neuraxial carcinoma.Molecular biology reports · 2020Review
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- Growth inhibition of human hepatocellular carcinoma cells by antagonism of the βOncology letters · 2018Article
- To block it, or not to block it?Journal of cancer research and clinical oncology · 2017Article
- Activation of β-adrenergic receptor promotes cellular proliferation in human glioblastoma.Oncology letters · 2017Article
- Concurrent activation of βCellular signalling · 2017Article
- Effects of 4(1H)-quinolinone derivative, a novel non-nucleotide allosteric purinergic P2YScientific reports · 2017Article
- Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.The Journal of pharmacology and experimental therapeutics · 2015Article
- Activation of β2-adrenergic receptor by (R,R')-4'-methoxy-1-naphthylfenoterol inhibits proliferation and motility of melanoma cells.Cellular signalling · 2015Article
- cAMP-Epac Pathway Stimulation Modulate Connexin-43 and MicroRNA-21 Expression in Glioma Cells.Basic and clinical neuroscience · 2015Article
- Systematic analysis of new drug indications by drug-gene-disease coherent subnetworks.CPT: pharmacometrics & systems pharmacology · 2014Article
- (R,R')-4'-methoxy-1-naphthylfenoterol targets GPR55-mediated ligand internalization and impairs cancer cell motility.Biochemical pharmacology · 2014Article
- β₂-adrenergic agonists modulate TNF-α induced astrocytic inflammatory gene expression and brain inflammatory cell populations.Journal of neuroinflammation · 2014Article
- Comparative molecular field analysis of fenoterol derivatives interacting with an agonist-stabilized form of the β₂-adrenergic receptor.Bioorganic & medicinal chemistry · 2014Article
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Authors and funding
8 authors at 4 institutions in 2 countries.
Funding
Abstract
Astrocytomas and glioblastomas have been particularly difficult to treat and refractory to chemotherapy. However, significant evidence has been presented that demonstrates a decrease in astrocytoma cell proliferation subsequent to an increase in cAMP levels. The 1321N1 astrocytoma cell line, as well as other astrocytomas and glioblastomas, expresses β(2)-adrenergic receptors (β(2)-ARs) that are coupled to G(s) activation and consequent cAMP production. Experiments were conducted to determine whether the β(2)-AR agonist (R,R')-fenoterol and other β(2)-AR agonists could attenuate mitogenesis and, if so, by what mechanism. Receptor binding studies were conducted to characterize β(2)-AR found in 1321N1 and U118 cell membranes. In addition, cells were incubated with (R,R')-fenoterol and analogs to determine their ability to stimulate intracellular cAMP accumulation and inhibit [(3)H]thymidine incorporation into the cells. 1321N1 cells contain significant levels of β(2)-AR as determined by receptor binding. (R,R')-fenoterol and other β(2)-AR agonists, as well as forskolin, stimulated cAMP accumulation in a dose-dependent manner. Accumulation of cAMP induced a decrease in [(3)H]thymidine incorporation. There was a correlation between concentration required to stimulate cAMP accumulation and inhibit [(3)H]thymidine incorporation. U118 cells have a reduced number of β(2)-ARs and a concomitant reduction in the ability of β(2)-AR agonists to inhibit cell proliferation. These studies demonstrate the efficacy of β(2)-AR agonists for inhibition of growth of the astrocytoma cell lines. Because a significant portion of brain tumors contain β(2)-ARs to a greater extent than whole brain, (R,R')-fenoterol, or some analog, may be useful in the treatment of brain tumors after biopsy to determine β(2)-AR expression.
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