Molecular Pharmacology and Structure of VPAC Receptors for VIP and PACAP

Regul Pept. 2002 Oct 15;108(2-3):165-73. doi: 10.1016/s0167-0115(02)00099-x.

Abstract

VIP and PACAP are two prominent neuropeptides which share two common G protein-coupled receptors VPAC1 and VPAC2 while PACAP has an additional specific receptor PAC1. This paper reviews the present knowledge regarding three aspects of VPAC receptors including: (i). receptor specificity towards natural VIP-related peptides and pharmacology of synthetic agonists or antagonists; (ii). receptor signaling; (iii). molecular basis of ligand-receptor interaction as determined by site-directed mutagenesis, construction of receptor chimeras and structural modeling.

Publication types

  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Humans
  • Ligands
  • Models, Molecular
  • Neuropeptides / physiology*
  • Pituitary Adenylate Cyclase-Activating Polypeptide
  • Protein Conformation
  • Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide
  • Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I
  • Receptors, Pituitary Hormone / physiology*
  • Receptors, Vasoactive Intestinal Peptide / chemistry
  • Receptors, Vasoactive Intestinal Peptide / physiology*
  • Receptors, Vasoactive Intestinal Peptide, Type II
  • Receptors, Vasoactive Intestinal Polypeptide, Type I
  • Substrate Specificity
  • Vasoactive Intestinal Peptide / chemistry
  • Vasoactive Intestinal Peptide / metabolism*

Substances

  • ADCYAP1 protein, human
  • ADCYAP1R1 protein, human
  • Ligands
  • Neuropeptides
  • Pituitary Adenylate Cyclase-Activating Polypeptide
  • Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide
  • Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I
  • Receptors, Pituitary Hormone
  • Receptors, Vasoactive Intestinal Peptide
  • Receptors, Vasoactive Intestinal Peptide, Type II
  • Receptors, Vasoactive Intestinal Polypeptide, Type I
  • VIPR1 protein, human
  • VIPR2 protein, human
  • Vasoactive Intestinal Peptide