Development of Selective Ligands for Pac1, Vpac1 and Vpac2 Receptors

摘要: At the time of its isolation, purification and sequencing in 1970-1972 by Said Mutt (Said Mutt, 1972;Mutt Said, 1974), VIP was third identified member a peptide group that included secretin (Mutt et al, 1970) glucagon (Bromer 1957). The family signature N-terminal histidylseryl sequence separated three amino acid residues from phenylalanylthreonyl sequence. Synthesis secretin, VIP, analogs as well careful study their biological activities revealed there no, or only negligible, interference with mediated responses, nor response. It also rapidly recognized shared common vitro properties each interacted cognate receptor other receptors (Bataille 1974; Robberecht 1976). established for peptides necessary high affinity recognition induction activity, C-terminus recognition. thus not possible to shorten significantly molecule without loss potency. This major point rational design agonists antagonists interest industry. Binding studies of125I-labeled characterized low sites were described (Christophe 1976; Laburthe 1978; Prieto 1979).