title: Bradykinin antagonists modified with dipeptide mimetic beta-turn inducers.
abstract: 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.
authors.affiliation: 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.
authors.forename: Maria C
authors.initials: MC
authors.lastname: Alcaro
authors.forename: Valerio
authors.initials: V
authors.lastname: Vinci
authors.forename: Anna M
authors.initials: AM
authors.lastname: D'Ursi
authors.forename: Mario
authors.initials: M
authors.lastname: Scrima
authors.forename: Mario
authors.initials: M
authors.lastname: Chelli
authors.forename: Sandro
authors.initials: S
authors.lastname: Giuliani
authors.forename: Stefania
authors.initials: S
authors.lastname: Meini
authors.forename: Marcello
authors.initials: M
authors.lastname: Di Giacomo
authors.forename: Lino
authors.initials: L
authors.lastname: Colombo
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Papini
mesh_terms: 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
chemical_list: D065094:Bradykinin B2 Receptor Antagonists; D004151:Dipeptides; C065679:icatibant; D001920:Bradykinin