NF546 [4,4′-(Carbonylbis(imino-3,1-phenylene-carbonylimino-3,1-(4-methyl-phenylene)-carbonylimino))-bis(1,3-xylene-α,α′-diphosphonic Acid) Tetrasodium Salt] Is a Non-Nucleotide P2Y11 Agonist and Stimulates Release of Interleukin-8 from Human Monocyte-Derived Dendritic Cells

• Published in: The Journal of pharmacology and experimental therapeutics Vol. 332; no. 1; pp. 238 - 247
• Main Authors: Meis, Sabine, Hamacher, Alexandra, Hongwiset, Darunee, Marzian, Claudia, Wiese, Michael, Eckstein, Niels, Royer, Hans-Dieter, Communi, Didier, Boeynaems, Jean-Marie, Hausmann, Ralf, Schmalzing, Günther, Kassack, Matthias U.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.01.2010; American Society for Pharmacology and Experimental Therapeutics
• Subjects: Calcium - metabolism; Cell Culture Techniques; Cell Line, Tumor; Cloning, Molecular; Cyclic AMP - metabolism; Dendritic Cells - drug effects; Dendritic Cells - immunology; Dendritic Cells - metabolism; Diphosphonates - pharmacology; Dose-Response Relationship, Drug; Humans; Interleukin-8 - metabolism; Ligands; Naphthalenesulfonates - pharmacology; Protein Binding; Purinergic P2 Receptor Agonists; Receptors, Purinergic P2 - metabolism; Receptors, Purinergic P2X; Recombinant Proteins; Transfection; Tricine; ATPγS; IL-4; IL-8; IL-12; LPS; NF157; DMEM; TSP-1; 2-MeSATP; NF546; ADPβS; NF340; BzATP; DC; ELISA

The G protein-coupled P2Y11 receptor is involved in immune system modulation. In-depth physiological evaluation is hampered, however, by a lack of selective and potent ligands. By screening a library of sulfonic and phosphonic acid derivatives at P2Y11 receptors recombinantly expressed in human 1321...