Identification of a pepducin acting as S1P3 receptor antagonist (pages 717–724)
Beatrice Severino, Giuseppina Maria Incisivo, Ferdinando Fiorino, Antonio Bertolino, Francesco Frecentese, Francesco Barbato, Serena Manganelli, Giada Maggioni, Domenica Capasso, Giuseppe Caliendo, Vincenzo Santagada, Raffaella Sorrentino, Fiorentina Roviezzo and Elisa Perissutti
Article first published online: 20 SEP 2013 | DOI: 10.1002/psc.2554
A novel peptidic S1P3 antagonist is described. Its ability to inhibit, in a dose-dependent manner, agonist-induced effects has been demonstrated in two different pharmacological models. The unique biological properties of the described antagonist make it a useful pharmacological tool for the study of S1P signaling involving the S1P3 receptor. Computational analysis suggested a correlation between specific conformations and activities.