Minimal structural requirements for agonist activity of PAR-2 activating peptides.
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)).
Santagada
Vincenzo
V
Department of Pharmaceutical Chemistry, University of Naples 'Federico II', Via D. Montesano 49, 80131, Naples, Italy.
Caliendo
Giuseppe
G
Severino
Beatrice
B
Perissutti
Elisa
E
Fiorino
Ferdinando
F
Cicala
Carla
C
De Filippis
Vincenzo
V
Cirino
Giuseppe
G
D000818:Animals; D001011:Aorta; D001120:Arginine / Q000737:chemistry; D004151:Dipeptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D007930:Leucine / Q000737:chemistry; D008297:Male; D015394:Molecular Structure; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D044464:Receptor, PAR-2; D018179:Receptors, Thrombin / Q000819:agonists*; D013329:Structure-Activity Relationship
D004151:Dipeptides; D044464:Receptor, PAR-2; D018179:Receptors, Thrombin; D001120:Arginine; D007930:Leucine