Maxadilan is a specific agonist and its deleted peptide (M65) is a specific antagonist for PACAP type 1 receptor

Ann N Y Acad Sci. 1998 Dec 11;865:253-8. doi: 10.1111/j.1749-6632.1998.tb11185.x.

Abstract

Maxadilan is a potent vasodilator peptide isolated from salivary glands extracts of the hematophagous sand fly. Recently, it was demonstrated that maxadilan binds to PACAP receptor type 1 in mammals, although maxadilan has no significant amino acid sequence homology with PACAP. In the present study, we demonstrated that maxadilan is a specific agonist of PACAP type 1 receptor (PACAP/VIP receptor 1; PVR1) as determined by the binding assay of [125I]PACAP27 and cAMP accumulation using CHO cells stably expressing PVR1, VIP1 receptor (PVR2), and VIP2 receptor (PVR3), and that the deleted peptide (#25-41) of maxadilan (termed as M65) is a specific antagonist of PVR1. In addition, maxadilan shares the binding sites for PACAP and stimulates cAMP in cultured rat cortical neurons. VIP stimulates cAMP accumulation probably through the binding to PVR1 since M65 blocks the VIP-induced cAMP accumulation in cultured rat cortical neurons.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • CHO Cells
  • Cells, Cultured
  • Cerebral Cortex / cytology
  • Cerebral Cortex / physiology
  • Cricetinae
  • Cyclic AMP / metabolism
  • Fetus
  • Insect Proteins / chemistry
  • Insect Proteins / pharmacology*
  • Molecular Sequence Data
  • Neurons / cytology
  • Neurons / drug effects
  • Neurons / physiology*
  • Neuropeptides / chemistry
  • Peptide Fragments / chemistry
  • Peptide Fragments / pharmacology*
  • Pituitary Adenylate Cyclase-Activating Polypeptide
  • Protein Structure, Secondary
  • Rats
  • Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide
  • Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I
  • Receptors, Pituitary Hormone / agonists
  • Receptors, Pituitary Hormone / antagonists & inhibitors
  • Receptors, Pituitary Hormone / genetics
  • Receptors, Pituitary Hormone / physiology*
  • Receptors, Vasoactive Intestinal Peptide / physiology
  • Receptors, Vasoactive Intestinal Peptide, Type II
  • Receptors, Vasoactive Intestinal Polypeptide, Type I
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / pharmacology
  • Reverse Transcriptase Polymerase Chain Reaction
  • Salivary Proteins and Peptides / chemistry
  • Salivary Proteins and Peptides / pharmacology
  • Sequence Alignment
  • Sequence Deletion
  • Sequence Homology, Amino Acid
  • Vasoactive Intestinal Peptide / chemistry

Substances

  • Adcyap1 protein, rat
  • Insect Proteins
  • Neuropeptides
  • Peptide Fragments
  • 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
  • Recombinant Proteins
  • Salivary Proteins and Peptides
  • maxadilan protein, insect
  • Vasoactive Intestinal Peptide
  • Cyclic AMP