ArticleThe Journal of pharmacology and experimental therapeutics2008
UDP is a competitive antagonist at the human P2Y14 receptor.
Article in The Journal of pharmacology and experimental therapeutics, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 56 citations in OpenAlex.
- Computational discovery and repurposing of chloramphenicol succinate as a potent P2YJournal of advanced research · 2026Article
- Involvement of uridine in brain and gut health: insights into its neuroprotective potential via the gut-brain axis.Pharmacological reports : PR · 2025Review
- Changes in P2YPhysiological reports · 2022Article
- Uridine Diphosphate Promotes Rheumatoid Arthritis Through P2Y6 Activation.Frontiers in pharmacology · 2021Article
- Role of UDP-Sugar Receptor P2YInternational journal of molecular sciences · 2020Article
- UDP-Sugars as Extracellular Signaling Molecules: Cellular and Physiologic Consequences of P2Y14 Receptor Activation.Molecular pharmacology · 2015Review
- The purinergic neurotransmitter revisited: a single substance or multiple players?Pharmacology & therapeutics · 2014Review
- Role of spinal P2Y6 and P2Y11 receptors in neuropathic pain in rats: possible involvement of glial cells.Molecular pain · 2014Article
- Novel vasocontractile role of the P2Y₁₄ receptor: characterization of its signalling in porcine isolated pancreatic arteries.British journal of pharmacology · 2014Article
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli.American journal of physiology. Cell physiology · 2013Article
- The nucleotide sugar UDP-glucose mobilizes long-term repopulating primitive hematopoietic cells.The Journal of clinical investigation · 2013Article
- A selective high-affinity antagonist of the P2Y14 receptor inhibits UDP-glucose-stimulated chemotaxis of human neutrophils.Molecular pharmacology · 2013Article
- Secretion of matrix metalloproteinase-9 from astrocytes by inhibition of tonic P2Y14-receptor-mediated signal(s).Cellular and molecular neurobiology · 2013Article
- P2Y receptor subtypes evoke different Ca2+ signals in cultured aortic smooth muscle cells.Purinergic signalling · 2012Article
- The UDP-sugar-sensing P2Y(14) receptor promotes Rho-mediated signaling and chemotaxis in human neutrophils.American journal of physiology. Cell physiology · 2012Article
- The impact of commercially available purinergic ligands on purinergic signalling research.Purinergic signalling · 2012Article
- Ca(2+) signalling by P2Y receptors in cultured rat aortic smooth muscle cells.British journal of pharmacology · 2010Article
- Signalling and pharmacological properties of the P2Y receptor.Acta physiologica (Oxford, England) · 2010Review
- Polyamidoamine (PAMAM) dendrimer conjugates of "clickable" agonists of the A3 adenosine receptor and coactivation of the P2Y14 receptor by a tethered nucleotide.Bioconjugate chemistry · 2010Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
G protein-coupled P2Y receptors (P2Y-R) are activated by adenine and uracil nucleotides. The P2Y(14) receptor (P2Y(14)-R) is activated by at least four naturally occurring UDP sugars, with UDP-glucose (UDP-Glc) being the most potent agonist. With the goal of identifying a competitive antagonist for the P2Y(14)-R, UDP was examined for antagonist activity in COS-7 cells transiently expressing the human P2Y(14)-R and a chimeric Galpha protein that couples Gi-coupled receptors to stimulation of phosphoinositide hydrolysis. UDP antagonized the agonist action of UDP-Glc, and Schild analysis confirmed that the antagonism was competitive (pK(B) = 7.28). Uridine 5'-O-thiodiphosphate also antagonized the human P2Y(14)-R (hP2Y(14)-R) with an apparent affinity similar to that of UDP. In contrast, no antagonist activity was observed with ADP, CDP, or GDP, and other uracil analogs also failed to exhibit antagonist activity. The antagonist activity of UDP was not observed at other hP2Y-R. In contrast to its antagonist action at the hP2Y(14)-R, UDP was a potent agonist (EC(50) = 0.35 muM) at the rat P2Y(14)-R. These results identify the first competitive antagonist of the P2Y(14)-R and demonstrate pharmacological differences between receptor orthologs.
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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.