ArticleJournal of medicinal chemistry2007
Structure-activity relationship of uridine 5'-diphosphoglucose analogues as agonists of the human P2Y14 receptor.
Article in Journal of medicinal chemistry, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
30 citing papers in PubMed, 64 citations in OpenAlex.
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- Design, Synthesis and Anti-Inflammation Evaluation ofDrug design, development and therapy · 2025Article
- Pharmacological characterization of P2Y receptor subtypes - an update.Purinergic signalling · 2024Review
- Article
- Structure-activity relationships of pyrimidine nucleotides containing a 5'-α,β-methylene diphosphonate at the P2YBioorganic & medicinal chemistry letters · 2021Article
- Discovery of novel and potent P2YJournal of advanced research · 2020Article
- UDP-sugars activate P2YVascular pharmacology · 2018Article
- New agents in HSC mobilization.International journal of hematology · 2017Review
- Nucleoside 5'-O-monophosphorothioates as modulators of the P2Y14 receptor and mast cell degranulation.Oncotarget · 2016Article
- Design, synthesis, pharmacological characterization of a fluorescent agonist of the P2Y₁₄ receptor.Bioorganic & medicinal chemistry letters · 2015Article
- Molecular modeling of the human P2Y14 receptor: A template for structure-based design of selective agonist ligands.Bioorganic & medicinal chemistry · 2015Article
- UDP-Sugars as Extracellular Signaling Molecules: Cellular and Physiologic Consequences of P2Y14 Receptor Activation.Molecular pharmacology · 2015Review
- Exploring a 2-naphthoic acid template for the structure-based design of P2Y14 receptor antagonist molecular probes.ACS chemical biology · 2014Article
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- Selective induction of P2Y14 receptor by RANKL promotes osteoclast formation.Molecules and cells · 2013Article
- The nucleotide sugar UDP-glucose mobilizes long-term repopulating primitive hematopoietic cells.The Journal of clinical investigation · 2013Article
- P2Y receptors in the mammalian nervous system: pharmacology, ligands and therapeutic potential.CNS & neurological disorders drug targets · 2012Review
- Development of a comprehensive set of P2 receptor pharmacological research compounds.Purinergic signalling · 2012Article
- Ca(2+) signalling by P2Y receptors in cultured rat aortic smooth muscle cells.British journal of pharmacology · 2010Article
- P2Y nucleotide receptors: promise of therapeutic applications.Drug discovery today · 2010Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
UDP-glucose (UDPG) and derivatives are naturally occurring agonists of the Gi protein-coupled P2Y14 receptor, which occurs in the immune system. We synthesized and characterized pharmacologically novel analogues of UDPG modified on the nucleobase, ribose, and glucose moieties, as the basis for designing novel ligands in conjunction with modeling. The recombinant human P2Y14 receptor expressed in COS-7 cells was coupled to phospholipase C through an engineered Galpha-q/i protein. Most modifications of the uracil or ribose moieties abolished activity; this is among the least permissive P2Y receptors. However, a 2-thiouracil modification in 15 (EC50 49 +/- 2 nM) enhanced the potency of UDPG (but not UDP-glucuronic acid) by 7-fold. 4-Thio analogue 13 was equipotent to UDPG, but S-alkylation was detrimental. Compound 15 was docked in a rhodposin-based receptor homology model, which correctly predicted potent agonism of UDP-fructose, UDP-mannose, and UDP-inositol. The hexose moiety of UDPG interacts with multiple H-bonding and charged residues and provides a fertile region for agonist modification.
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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.