Pyrimidine Ribonucleotides with Enhanced Selectivity as P2Y(6) Receptor Agonists: Novel 4-Alkyloxyimino, (S)-Methanocarba, and 5′-Triphosphate γ-Ester Modifications

The P2Y(6) receptor is a cytoprotective G protein-coupled receptor (GPCR) activated by UDP (EC(50), 0.30 μM). We compared and combined modifications to enhance P2Y(6) receptor agonist selectivity, including ribose ring constraint, 5-iodo and 4-alkyloxyimino modifications, and phosphate modifications...

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Hauptverfasser: Maruoka, Hiroshi, Barrett, Matthew O., Ko, Hyojin, Tosh, Dilip K., Melman, Artem, Burianek, Lauren E., Balasubramanian, Ramachandran, Berk, Barkin, Costanzi, Stefano, Harden, T. Kendall, Jacobson, Kenneth A.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2010
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC2935147/
https://ncbi.nlm.nih.gov/pubmed/20446735
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm100287t
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