Investigation of the interaction of VIP binding sites with VIP and PACAP in human brain

Neurosci Lett. 1992 Mar 16;137(1):19-23. doi: 10.1016/0304-3940(92)90288-i.

Abstract

We have compared the binding of [125I]vasoactive intestinal polypeptide (VIP) to human brain membranes with that of [125I]PACAP27. [125I]VIP was displaced by PACAP27, VIP and two synthetic peptides, peptide-1 (N-terminal PACAP27/C-terminal VIP) and peptide-2 (N-terminal VIP/C-terminal PACAP27), but the IC50 of PACAP27 and peptide-1 were 10-20 times lower than those of VIP and peptide-2. [125I]PACAP27 was readily displaced by PACAP27 and peptide-1, with an IC50 of less than 1 nM, but poorly by VIP and peptide-2. Chemical cross-linking revealed that both labels were bound to polypeptides of Mr 66,000 and Mr 50,000. The results indicate that in human brain membranes both binding sites have a higher affinity to the N-terminal sequence of PACAP27, and VIP binding sites prefer PACAP27 to VIP itself.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Amino Acid Sequence
  • Humans
  • Molecular Sequence Data
  • Neuropeptides / metabolism*
  • Peptide Fragments / metabolism
  • Pituitary Adenylate Cyclase-Activating Polypeptide
  • Receptors, Cell Surface / metabolism*
  • Receptors, Gastrointestinal Hormone / metabolism*
  • Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide
  • Receptors, Pituitary Hormone*
  • Receptors, Vasoactive Intestinal Peptide

Substances

  • ADCYAP1 protein, human
  • Neuropeptides
  • Peptide Fragments
  • Pituitary Adenylate Cyclase-Activating Polypeptide
  • Receptors, Cell Surface
  • Receptors, Gastrointestinal Hormone
  • Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide
  • Receptors, Pituitary Hormone
  • Receptors, Vasoactive Intestinal Peptide
  • Adenylyl Cyclases