Increase of VPAC receptor s binding to the 16g-glutamyl diaminopropane vasoactive intestinal peptide (VIP-DAP) agonist, a vasoactive intestinal polypeptide (VIP) structural analog contg. a pos. charge at position 16, has confirmed the importance of a pos. charge at this site. By investigating the effect of distance from the peptide backbone Ca of a pos. charge in position 16, data are reported here concerning: (i) a novel chem. method used for the synthesis of a new family of 16g-glutamyl diamine VIP derivs. 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 compds. 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 deriv. 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.
Effect of positive charge in VIP 16g-glutamyl diamino derivatives on hVPAC1 and hVPAC2 receptor function / S., De Maria; V., Metafora; S., Metafora; G., Ravagnan; M., Carteni; G., Pontoni; A., Facchiano; M., Lepretti; Severino, Beatrice; Caliendo, Giuseppe; Santagada, Vincenzo; I., Langer; P. R. o. b. b. e. r. e. c. h., T.. - In: JOURNAL OF PEPTIDE SCIENCE. - ISSN 1075-2617. - STAMPA. - 14(1):(2008), pp. 102-109.
Effect of positive charge in VIP 16g-glutamyl diamino derivatives on hVPAC1 and hVPAC2 receptor function
SEVERINO, BEATRICE;CALIENDO, GIUSEPPE;SANTAGADA, VINCENZO;
2008
Abstract
Increase of VPAC receptor s binding to the 16g-glutamyl diaminopropane vasoactive intestinal peptide (VIP-DAP) agonist, a vasoactive intestinal polypeptide (VIP) structural analog contg. a pos. charge at position 16, has confirmed the importance of a pos. charge at this site. By investigating the effect of distance from the peptide backbone Ca of a pos. charge in position 16, data are reported here concerning: (i) a novel chem. method used for the synthesis of a new family of 16g-glutamyl diamine VIP derivs. 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 compds. 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 deriv. 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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
