Bradykinin antagonists modified with dipeptide mimetic beta-turn inducers.
Bradykinin (BK) is involved in a wide variety of pathophysiological processes. Potent BK peptide antagonists can be developed introducing constrained unnatural amino acids, necessary to force the secondary structure of the molecule. In this paper, we report a structure-activity relationship study of two peptide analogues of the potent B2 antagonist HOE 140 by replacing the D-Tic-Oic dipeptide with conformationally constrained dipeptide mimetic beta-turn inducers.
Alcaro
Maria C
MC
Laboratory of Peptide and Protein Chemistry and Biology, Dipartimento di Chimica Organica, University of Firenze and CNR-ICCOM, Polo Scientifico, Via della Lastruccia 13, I-50019 Sesto Fiorentino (FI), Italy.
Vinci
Valerio
V
D'Ursi
Anna M
AM
Scrima
Mario
M
Chelli
Mario
M
Giuliani
Sandro
S
Meini
Stefania
S
Di Giacomo
Marcello
M
Colombo
Lino
L
Papini
Anna Maria
AM
D001920:Bradykinin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D065094:Bradykinin B2 Receptor Antagonists; D004151:Dipeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D008968:Molecular Conformation; D018716:Molecular Mimicry; D017433:Protein Structure, Secondary; D013329:Structure-Activity Relationship
D065094:Bradykinin B2 Receptor Antagonists; D004151:Dipeptides; C065679:icatibant; D001920:Bradykinin