ArticleBiochemical pharmacology2010
UDP-glucose acting at P2Y14 receptors is a mediator of mast cell degranulation.
Article in Biochemical pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers.
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Who cites it
45 citing papers in PubMed, 78 citations in OpenAlex.
- Computational discovery and repurposing of chloramphenicol succinate as a potent P2YJournal of advanced research · 2026Article
- P2YACS pharmacology & translational science · 2025Article
- Drug-like Antagonists of P2Y Receptor Subtypes: An Update.Journal of medicinal chemistry · 2025Review
- 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
- Physiologic roles of P2 receptors in leukocytes.Journal of leukocyte biology · 2022Review
- Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2YJournal of medicinal chemistry · 2022Article
- Chemogenetic stimulation of the GPharmacology research & perspectives · 2021Article
- Review
- Purinergic receptors in airway hydration.Biochemical pharmacology · 2021Review
- P2Y14 Receptor as a Target for Neutrophilia Attenuation in Severe COVID-19 Cases: From Hematopoietic Stem Cell Recruitment and Chemotaxis to Thrombo-inflammation.Stem cell reviews and reports · 2021Review
- Exploration of Alternative Scaffolds for P2YJournal of medicinal chemistry · 2020Article
- Discovery of novel and potent P2YJournal of advanced research · 2020Article
- Role of UDP-Sugar Receptor P2YInternational journal of molecular sciences · 2020Article
- Glycogen metabolism regulates macrophage-mediated acute inflammatory responses.Nature communications · 2020Article
- Structure-Guided Modification of Heterocyclic Antagonists of the P2YJournal of medicinal chemistry · 2018Article
- UDP-sugars activate P2YVascular pharmacology · 2018Article
- Peripheral inflammatory pain sensitisation is independent of mast cell activation in male mice.Pain · 2017Article
- Gene-based analysis of regulatory variants identifies 4 putative novel asthma risk genes related to nucleotide synthesis and signaling.The Journal of allergy and clinical immunology · 2017Article
- Purinergic Signaling in Mast Cell Degranulation and Asthma.Frontiers in pharmacology · 2017Review
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 1 country.
Funding
Abstract
UDP-glucose (UDPG), a glycosyl donor in the biosynthesis of carbohydrates, is an endogenous agonist of the G protein-coupled P2Y(14) receptor. RBL-2H3 mast cells endogenously express a P2Y(14) receptor at which UDPG mediates degranulation as indicated by beta-hexosaminidase (HEX) release. Both UDPG and a more potent, selective 2-thio-modified UDPG analog, MRS2690 (diphosphoric acid 1-alpha-d-glucopyranosyl ester 2-[(2-thio)uridin-5''-yl] ester), caused a substantial calcium transient in RBL-2H3 cells, which was blocked by pertussis toxin, indicating the presence of the G(i)-coupled P2Y(14) receptor, supported also by quantitative detection of abundant mRNA. Expression of the closely related P2Y(6) receptor was over 100 times lower than the P2Y(14) receptor, and the P2Y(6) agonist 3-phenacyl-UDP was inactive in RBL-2H3 cells. P2Y(14) receptor agonists also induced [(35)S]GTPgammaS binding to RBL-2H3 cell membranes, and phosphorylation of ERK1/2, P38 and JNK. UDPG and MRS2690 concentration-dependently enhanced HEX release with EC(50) values of 1150+/-320 and 103+/-18nM, respectively. The enhancement was completely blocked by pertussis toxin and significantly diminished by P2Y(14) receptor-specific siRNA. Thus, mast cells express an endogenous P2Y(14) receptor, which mediates G(i)-dependent degranulation and is therefore a potential novel therapeutic target for allergic conditions.
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Registered trials
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.