Protease-activated receptor 2 (PAR-2) is involved in inflammatory, gastrointestinal, and vascular diseases. The aim of the present work was to elucidate the minimal structural features for PAR-2 agonist activity in short peptides. Our study resulted in the discovery of dipeptide derivatives of N(alpha)-benzoyl-Arg(NO(2))-Leu-NH(2) displaying a potency comparable to that of the full-length rat PAR-2 activating peptide (Ser-Leu-Ile-Gly-Arg-Leu-NH(2)).
Minimal structural requirements for agonist activity of PAR-2 activating peptides / Santagada, Vincenzo; Caliendo, Giuseppe; Severino, Beatrice; Perissutti, Elisa; Fiorino, Ferdinando; Cicala, Carla; De Filippis, V; Cirino, Giuseppe. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 12:1(2002), pp. 21-24.
Minimal structural requirements for agonist activity of PAR-2 activating peptides.
SANTAGADA, VINCENZO;CALIENDO, GIUSEPPE;SEVERINO, BEATRICE;PERISSUTTI, ELISA;FIORINO, FERDINANDO;CICALA, CARLA;CIRINO, GIUSEPPE
2002
Abstract
Protease-activated receptor 2 (PAR-2) is involved in inflammatory, gastrointestinal, and vascular diseases. The aim of the present work was to elucidate the minimal structural features for PAR-2 agonist activity in short peptides. Our study resulted in the discovery of dipeptide derivatives of N(alpha)-benzoyl-Arg(NO(2))-Leu-NH(2) displaying a potency comparable to that of the full-length rat PAR-2 activating peptide (Ser-Leu-Ile-Gly-Arg-Leu-NH(2)).I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
