title: Novel nucleotide triphosphates as potent P2Y2 agonists with enhanced stability over UTP.
abstract: The synthesis of a series of novel C-linked nucleotide triphosphates is reported. These exhibit excellent agonist potency and selectivity for the P2Y2 receptor with a number of examples having EC50 values below 10 nM. Representative compounds from the N-linked and C-linked series showed enhanced metabolic stability compared with that of the natural ligand UTP.
authors.affiliation: UCB-Group, Granta Park, Abington, Cambridge CB1 6GS, UK. richard.davenport@ucb-group.com
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Davenport
authors.forename: Paloma
authors.initials: P
authors.lastname: Diaz
authors.forename: Frances C A
authors.initials: FC
authors.lastname: Galvin
authors.forename: Steve
authors.initials: S
authors.lastname: Lloyd
authors.forename: Stephen R
authors.initials: SR
authors.lastname: Mack
authors.forename: Ray
authors.initials: R
authors.lastname: Owens
authors.forename: Verity
authors.initials: V
authors.lastname: Sabin
authors.forename: Joanne
authors.initials: J
authors.lastname: Wynn
mesh_terms: D045744:Cell Line, Tumor; D002853:Chromatography, Liquid; D006801:Humans; D007202:Indicators and Reagents; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D009711:Nucleotides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D058910:Purinergic P2 Receptor Agonists; D058473:Receptors, Purinergic P2Y2; D011994:Recombinant Proteins; D013056:Spectrophotometry, Ultraviolet; D014544:Uridine Triphosphate / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D007202:Indicators and Reagents; D008024:Ligands; D009711:Nucleotides; C546385:P2RY2 protein, human; D058910:Purinergic P2 Receptor Agonists; D058473:Receptors, Purinergic P2Y2; D011994:Recombinant Proteins; D014544:Uridine Triphosphate