ArticleEuropean journal of medicinal chemistry2009
Identification of hydrolytically stable and selective P2Y(1) receptor agonists.
Article in European journal of medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 24 citations in OpenAlex.
- Nucleotide P2YPurinergic signalling · 2020Article
- Overview of Biologically Active Nucleoside Phosphonates.Frontiers in chemistry · 2020Review
- Highly potent and selective ectonucleotide pyrophosphatase/phosphodiesterase I inhibitors based on an adenosine 5'-(α or γ)-thio-(α,β- or β,γ)-methylenetriphosphate scaffold.Journal of medicinal chemistry · 2014Article
- Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist.Journal of medicinal chemistry · 2012Article
- P2Y receptors in the mammalian nervous system: pharmacology, ligands and therapeutic potential.CNS & neurological disorders drug targets · 2012Review
- Pharmacochemistry of the platelet purinergic receptors.Purinergic signalling · 2011Article
- Pyrimidine ribonucleotides with enhanced selectivity as P2Y(6) receptor agonists: novel 4-alkyloxyimino, (S)-methanocarba, and 5'-triphosphate gamma-ester modifications.Journal of medicinal chemistry · 2010Article
- 2-MeS-beta,gamma-CCl2-ATP is a potent agent for reducing intraocular pressure.Journal of medicinal chemistry · 2010Article
- A novel insulin secretagogue based on a dinucleoside polyphosphate scaffold.Journal of medicinal chemistry · 2010Article
- Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups.Journal of medicinal chemistry · 2010Article
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Authors and funding
7 authors at 4 institutions in 3 countries.
Funding
Abstract
P2Y nucleotide receptors (P2YRs) are attractive pharmaceutical targets. Most P2YR agonists proposed as drugs consist of a nucleotide scaffold, but their use is limited due to their chemical and enzymatic instabilities. To identify drug candidates, we developed non-hydrolyzable P2YR agonists. We synthesized ATP-beta,gamma-CH(2) analogues 2-4, and evaluated their chemical and metabolic stabilities and activities at P2Y(1,2,4,6) receptors. Analogues 2-4 exhibited t(1/2) values of 14.5-65 h in gastric juice pH. They were completely resistant to alkaline phosphatase for 30 min at 37 degrees C and slowly hydrolyzed in human blood serum (t(1/2) 12.7-71.9 h). In comparison to ATP, analogues 2-4 were barely hydrolyzed by nucleoside triphosphate diphosphohydrolases, NTPDase1,2,3,8 (< 8% hydrolysis), and nucleotide pyrophosphatases, NPP1,3 (< or = 10% hydrolysis). Analogues 2 and 4B were selective agonists of the P2Y(1)R with EC(50)s of 0.08 and 17.2 microM, respectively. These features make analogues 2 and 4B potential therapeutic agents for health disorders involving the P2Y(1)R.
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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.