ArticleBritish journal of pharmacology2010
The ecto-nucleotidase NTPDase1 differentially regulates P2Y1 and P2Y2 receptor-dependent vasorelaxation.
Article in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 53 citations in OpenAlex.
- Integrating multi-omics, machine learning, and molecular dynamics simulations to identify glutamate metabolism-related biomarkers and drug candidates in rheumatoid arthritis.Frontiers in molecular biosciences · 2026Article
- Impact of Estrogen on Purinergic Signaling in Microvascular Disease.International journal of molecular sciences · 2025Review
- Migraine signaling pathways: purine metabolites that regulate migraine and predispose migraineurs to headache.Molecular and cellular biochemistry · 2023Review
- NTPDase1/CD39 Ectonucleotidase Is Necessary for Normal Arterial Diameter Adaptation to Flow.International journal of molecular sciences · 2023Article
- Synthesis and biological evaluation of sulfamoyl benzamide derivatives as selective inhibitors forRSC advances · 2023Article
- The Interplay of Endothelial P2Y Receptors in Cardiovascular Health: From Vascular Physiology to Pathology.International journal of molecular sciences · 2022Review
- Thrombo-Inflammation: A Focus on NTPDase1/CD39.Cells · 2021Review
- Human Pannexin 1 channel: Insight in structure-function mechanism and its potential physiological roles.Molecular and cellular biochemistry · 2021Review
- Loss of vascular expression of nucleoside triphosphate diphosphohydrolase-1/CD39 in hypertension.Purinergic signalling · 2018Article
- P2YFrontiers in pharmacology · 2018Article
- The Impact of Purinergic System Enzymes on Noncommunicable, Neurological, and Degenerative Diseases.Journal of immunology research · 2018Review
- The role of purinergic signaling in the etiology of migraine and novel antimigraine treatment.Purinergic signalling · 2015Review
- Cellular mechanisms of tissue fibrosis. 6. Purinergic signaling and response in fibroblasts and tissue fibrosis.American journal of physiology. Cell physiology · 2014Review
- Ticlopidine in its prodrug form is a selective inhibitor of human NTPDase1.Mediators of inflammation · 2014Article
- Ecto-nucleoside triphosphate diphosphohydrolase 2 modulates local ATP-induced calcium signaling in human HaCaT keratinocytes.PloS one · 2013Article
- Cellular function and molecular structure of ecto-nucleotidases.Purinergic signalling · 2012Review
- Mechanisms of ATP release and signalling in the blood vessel wall.Cardiovascular research · 2012Review
- Ectonucleotide triphosphate diphosphohydrolase-1 (CD39) mediates resistance to occlusive arterial thrombus formation after vascular injury in mice.The American journal of pathology · 2012Article
- Pannexin 1 in the regulation of vascular tone.Trends in cardiovascular medicine · 2012Review
- Expression of pannexin isoforms in the systemic murine arterial network.Journal of vascular research · 2012Article
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Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
Abstract
background and purposeExtracellular nucleotides produce vasodilatation through endothelial P2 receptor activation. As these autacoids are actively metabolized by the ecto-nucleotidase nucleoside triphosphate diphosphohydrolase-1 (NTPDase1), we studied the effects of this cell surface enzyme on nucleotide-dependent vasodilatation. EXPERIMENTAL APPROACH: Vascular NTPDase expression and activity were evaluated by immunohistochemistry and histochemistry. The vascular effects of nucleotides were tested in vivo by monitoring mean arterial pressure, and in vitro comparing reactivity of aortic rings using wild-type and Entpd1(-/-) (lacking NTPDase1) mice. KEY
resultsThe absence of NTPDase1 in Entpd1(-/-) mice led to a dramatic drop in endothelial nucleotidase activity. This deficit was associated with an exacerbated decrease in blood pressure after nucleotide injection. Following ATP injection, mean arterial pressure was decreased in Entpd1(+/+) and Entpd1(-/-) mice by 5.0 and 17%, respectively, and by 0.1 and 19% after UTP injection (10 nmole.kg(-1) both). In vitro, the concentration-response curves of relaxation to ADP and ATP were shifted to the left, revealing a facilitation of endothelial P2Y1 and P2Y2 receptor activation in Entpd1(-/-) mice. EC(50) values in Entpd1(+/+) versus Entpd1(-/-) aortic rings were 14 microM versus 0.35 microM for ADP, and 29 microM versus 1 microM for ATP. In Entpd1(-/-) aortas, P2Y1 receptors were more extensively desensitized than P2Y2 receptors. Relaxations to the non-hydrolysable analogues ADPbetaS (P2Y1) and ATPgammaS (P2Y2) were equivalent in both genotypes confirming the normal functionality of these P2Y receptors in mutant mice. CONCLUSIONS AND IMPLICATIONS: NTPDase1 controls endothelial P2Y receptor-dependent relaxation, regulating both agonist level and P2 receptor reactivity.
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