Bradykinin antagonists modified with dipeptide mimetic beta-turn inducers |
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| Authors: | Alcaro Maria C Vinci Valerio D'Ursi Anna M Scrima Mario Chelli Mario Giuliani Sandro Meini Stefania Di Giacomo Marcello Colombo Lino Papini Anna Maria |
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| Institution: | 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. |
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| 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. |
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