ArticleMolecular pharmacology2013
A selective high-affinity antagonist of the P2Y14 receptor inhibits UDP-glucose-stimulated chemotaxis of human neutrophils.
Article in Molecular pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers.
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Who cites it
59 citing papers in PubMed, 111 citations in OpenAlex.
- Nucleotide signaling in neutrophils: a key player in cancer dynamics.Purinergic signalling · 2026Review
- Computational discovery and repurposing of chloramphenicol succinate as a potent P2YJournal of advanced research · 2026Article
- P2Y14 receptor activation and neutrophil signaling: linking inflammation to systemic pathophysiology.Purinergic signalling · 2026Review
- UDP-glucose regulates dendritic cell mitochondrial respiration via a nitric oxide-dependent mechanism.Journal of leukocyte biology · 2025Article
- Design, Synthesis and Anti-Inflammation Evaluation ofDrug design, development and therapy · 2025Article
- Pharmacological interaction and immune response of purinergic receptors in therapeutic modulation.Purinergic signalling · 2024Review
- Differently expression of the metabotropic P2Y receptor family after hypoxia-induced seizures in neonates and seizure suppression via P2YPurinergic signalling · 2024Article
- Pharmacological characterization of P2Y receptor subtypes - an update.Purinergic signalling · 2024Review
- Article
- Uridine Diphosphate Glucose (UDP-G) Activates Oxidative Stress and Respiratory Burst in Isolated Neutrophils.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Alicyclic Ring Size Variation of 4-Phenyl-2-naphthoic Acid Derivatives as P2YJournal of medicinal chemistry · 2023Article
- Effects of uridine and nucleotides on hemostasis parameters.Journal of thrombosis and thrombolysis · 2023Article
- A host defense peptide mimetic, brilacidin, potentiates caspofungin antifungal activity against human pathogenic fungi.Nature communications · 2023Article
- Reduced urine volume and changed renal sphingolipid metabolism in P2ry14-deficient mice.Frontiers in cell and developmental biology · 2023Article
- Physiologic roles of P2 receptors in leukocytes.Journal of leukocyte biology · 2022Review
- A novel definition and treatment of hyperinflammation in COVID-19 based on purinergic signalling.Purinergic signalling · 2022Review
- Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2YJournal of medicinal chemistry · 2022Article
- Naringin Relieves Diabetic Cardiac Autonomic Neuropathy Mediated by P2YFrontiers in pharmacology · 2022Article
- GPR105-Targeted Therapy Promotes Gout Resolution as a Switch Between NETosis and Apoptosis of Neutrophils.Frontiers in immunology · 2022Article
- Recommended tool compounds and drugs for blocking P2X and P2Y receptors.Purinergic signalling · 2021Review
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
The nucleotide-sugar-activated P2Y14 receptor (P2Y14-R) is highly expressed in hematopoietic cells. Although the physiologic functions of this receptor remain undefined, it has been strongly implicated recently in immune and inflammatory responses. Lack of availability of receptor-selective high-affinity antagonists has impeded progress in studies of this and most of the eight nucleotide-activated P2Y receptors. A series of molecules recently were identified by Gauthier et al. (Gauthier et al., 2011) that exhibited antagonist activity at the P2Y14-R. We synthesized one of these molecules, a 4,7-disubstituted 2-naphthoic acid derivative (PPTN), and studied its pharmacological properties in detail. The concentration-effect curve of UDP-glucose for promoting inhibition of adenylyl cyclase in C6 glioma cells stably expressing the P2Y14-R was shifted to the right in a concentration-dependent manner by PPTN. Schild analyses revealed that PPTN-mediated inhibition followed competitive kinetics, with a KB of 434 pM observed. In contrast, 1 μM PPTN exhibited no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. UDP-glucose-promoted chemotaxis of differentiated HL-60 human promyelocytic leukemia cells was blocked by PPTN with a concentration dependence consistent with the KB determined with recombinant P2Y14-R. In contrast, the chemotactic response evoked by the chemoattractant peptide fMetLeuPhe was unaffected by PPTN. UDP-glucose-promoted chemotaxis of freshly isolated human neutrophils also was blocked by PPTN. In summary, this work establishes PPTN as a highly selective high-affinity antagonist of the P2Y14-R that is useful for interrogating the action of this receptor in physiologic systems.
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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.