In this paper we reported the synthesis and the in vitro and the in vivo biological evaluation of linear pseudo-peptides incorporating the N-VGCC blocker tripeptide Phe-NMe-Leu-Tyr(OBz)-NtBu and the biphalin pharmacophore Tyr-D-Ala-Gly-Phe. The novel sequences have been designed by using amino acids of different length to join the two pharmacophores and explore the structure–activity relationships of the novel compounds.
Design, synthesis and biological profile of mixed opioid agonist/N-VGCC blocker peptides / Stefanucci, Azzurra; Novellino, Ettore; Macedonio, Giorgia; Dimmito, Marilisa Pia; Mirzaie, Sako; Caldas Cardoso, Fernanda; Lewis, Richard; Zádor, Ferenc; Erdei, Anna I.; Dvorácskó, Szabolcs; Tömböly, Csaba; Benyhe, Sandor; Pieretti, Stefano; Minosi, Paola; Mollica, Adriano. - In: NEW JOURNAL OF CHEMISTRY. - ISSN 1369-9261. - 42:8(2018), pp. 5656-5659. [10.1039/C7NJ04969B]
Design, synthesis and biological profile of mixed opioid agonist/N-VGCC blocker peptides
Pieretti, Stefano;Minosi, Paola;Mollica, AdrianoUltimo
2018
Abstract
In this paper we reported the synthesis and the in vitro and the in vivo biological evaluation of linear pseudo-peptides incorporating the N-VGCC blocker tripeptide Phe-NMe-Leu-Tyr(OBz)-NtBu and the biphalin pharmacophore Tyr-D-Ala-Gly-Phe. The novel sequences have been designed by using amino acids of different length to join the two pharmacophores and explore the structure–activity relationships of the novel compounds.| File | Dimensione | Formato | |
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