ArticleBritish journal of pharmacology2007
Specificity of the ecto-ATPase inhibitor ARL 67156 on human and mouse ectonucleotidases.
Article in British journal of pharmacology, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 101 papers.
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Who cites it
101 citing papers in PubMed, 204 citations in OpenAlex.
- Cell stress increases ATP release in NLRP3 inflammasome-mediated autoinflammatory diseases, resulting in cytokine imbalance.Proceedings of the National Academy of Sciences of the United States of America · 2015Trial
- NTPDase2 suppresses hippocampal astrocyte-supplied cholesterol through hydrolyzing eATP in depression.Molecular psychiatry · 2026Article
- Nucleotide-Derived Competitive Inhibitors of Ectonucleotidase CD39─A Promising Extracellular Target for Immunotherapy of Cancer.Journal of medicinal chemistry · 2026Article
- ENTPD3 as a novel regulator of endometrial receptivity: suppressing EMT via the ATP-P2Y2 axis in patients with recurrent implantation failure.Cellular & molecular biology letters · 2026Article
- Proteasomal-dependent endothelial P2YPurinergic signalling · 2026Article
- CD39 polymorphism enables lung thrombosis in sickle cell disease.Nature communications · 2026Article
- CD39 activities in the treated acupoints contributed to the analgesic mechanism of acupuncture on arthritis rats.Purinergic signalling · 2025Article
- Synthesis, Characterization, Interactions, and Immunomodulatory Function of Ectonucleotidase CD39/CD73 Inhibitor 8-Butylthioadenosine 5'-Monophosphate.ACS pharmacology & translational science · 2025Article
- Ectonucleotidase inhibitors: targeting signaling pathways for therapeutic advancement-an in-depth review.Purinergic signalling · 2025Review
- Nanomedicines harnessing cGAS-STING pathway: sparking immune revitalization to transform 'cold' tumors into 'hot' tumors.Molecular cancer · 2024Review
- Regulatory role of CD39 and CD73 in tumor immunity.Future oncology (London, England) · 2024Review
- Article
- Synthesis of new class of indole acetic acid sulfonate derivatives as ectonucleotidases inhibitors.RSC advances · 2023Article
- Synthesis and biological evaluation of sulfamoyl benzamide derivatives as selective inhibitors forRSC advances · 2023Article
- The real-time detection of acupuncture-induced extracellular ATP mobilization in acupoints and exploration of its role in acupuncture analgesia.Purinergic signalling · 2023Article
- Dual Role of the P2X7 Receptor in Dendritic Outgrowth during Physiological and Pathological Brain Development.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2023Article
- Spatial mapping of ectonucleotidase gene expression in the murine urinary bladder.Frontiers in physiology · 2023Article
- Heparins are potent inhibitors of ectonucleotide pyrophosphatase/phospho-diesterase-1 (NPP1) - a promising target for the immunotherapy of cancer.Frontiers in immunology · 2023Article
- Shedding Light on the Role of Na,K-ATPase as a Phosphatase during Matrix-Vesicle-Mediated Mineralization.International journal of molecular sciences · 2022Article
- Protein kinase inhibitor ceritinib blocks ectonucleotidase CD39 - a promising target for cancer immunotherapy.Journal for immunotherapy of cancer · 2022Article
41 more citing papers are in PubMed but not listed here.
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
background and purposeARL 67156, 6-N,N-Diethyl-D-beta-gamma-dibromomethylene adenosine triphosphate, originally named FPL 67156, is the only commercially available inhibitor of ecto-ATPases. Since the first report on this molecule, various ectonucleotidases responsible for the hydrolysis of ATP at the cell surface have been cloned and characterized. In this work, we identified the ectonucleotidases inhibited by ARL 67156. EXPERIMENTAL APPROACH: The effect of ARL 67156 on recombinant NTPDase1, 2, 3 & 8 (mouse and human), NPP1, NPP3 and ecto-5'-nucleotidase (human) have been evaluated. The inhibition of the activity of NTPDases (using the following substrates: ATP, ADP, UTP), NPPs (pnp-TMP, Ap(3)A) and ecto-5'-nucleotidase (AMP) was measured by colorimetric or HPLC assays. KEY
resultsARL 67156 was a weak competitive inhibitor of human NTPDase1, NTPDase3 and NPP1 with K(i) of 11+/-3, 18+/-4 and 12+/-3 microM, respectively. At concentrations used in the literature (50-100 microM), ARL 67156 partially but significantly inhibited the mouse and human forms of these enzymes. NTPDase2, NTPDase8, NPP3 and ecto-5'-nucleotidase activities were less affected. Importantly, ARL 67156 was not hydrolysed by either human NTPDase1, 2, 3, 8, NPP1 or NPP3. CONCLUSIONS AND IMPLICATIONS: In cell environments where NTPDase1, NTPDase3, NPP1 or mouse NTPDase8 are present, ARL 67156 would prolong the effect of endogenously released ATP on P2 receptors. However, it does not block any ectonucleotidases efficiently when high concentrations of substrates are present, such as in biochemical, pharmacological or P2X(7) assays. In addition, ARL 67156 is not an effective inhibitor of NTPDase2, human NTPDase8, NPP3 and ecto-5'-nucleotidase.
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