Salvatore de Maria,
Vittoria Metafora,
Salvatore Metafora,
Gianpietro Ravagnan, Maria Cartení,
Gabriele Pontoni,
Angelo Facchiano,
Marilena Lepretti,
Beatrice Severino,
Giuseppe Caliendo,
Vincenzo Santagada,
Ingrid Langer,
Patrick Robberecht
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ABSTRACT: Increase of VPAC receptor s binding to the 16γ-glutamyl diaminopropane vasoactive intestinal peptide (VIP-DAP) agonist, a vasoactive intestinal polypeptide (VIP) structural analogue containing a positive charge at position 16, has confirmed the importance of a positive charge at this site. By investigating the effect of distance from the peptide backbone Cα of a positive charge in position 16, data are reported here concerning: (i) a novel chemical method used for the synthesis of a new family of 16γ-glutamyl diamine VIP derivatives differing among them for single carbon atoms and including diaminoethane (VIP-DAE2), diaminopropane (VIP-DAP3), diaminobutane (VIP-DAB4), diaminopentane (VIP-DAP5), and diaminohexane (VIP-DAH6); (ii) functional characterization of these compounds on human VPAC1 and VPAC2 receptors. In more detail, the EC50 and IC50 values, when measured as a function of the alkylic chain length, show in more detail, that the use of VIP-DAB4 derivative changes the IC50 but not the EC50, thus indicating on hVPAC2 receptor an unexpected relationship between binding and activity that differs from that obtained on hVPAC1. Copyright © 2007 European Peptide Society and John Wiley & Sons, Ltd.
Journal of Peptide Science 09/2007; 14(1):102 - 109. · 1.80 Impact Factor
