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 b-turn inducers.
Bradykinin antagonists modified with dipeptide mimetic beta-turn inducers / M.C. ALCARO; V. VINCI; A.M. DURSI; M. SCRIMA; M. CHELLI; S. GIULIANI; S. MEINI; M. DI GIACOMO; L. COLOMBO; A.M. PAPINI. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 16:(2006), pp. 2387-2390. [10.1016/j.bmcl.2006.01.125]
Bradykinin antagonists modified with dipeptide mimetic beta-turn inducers
M. C. ALCARO;M. CHELLI;PAPINI, ANNA MARIA
2006
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 b-turn inducers.
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