Characterization of the new photoaffinity probe (Bz2-K24)-VIP

Ann N Y Acad Sci. 2006 Jul:1070:575-80. doi: 10.1196/annals.1317.084.

Abstract

Site-directed mutagenesis and molecular modeling demonstrated that the N-terminal ectodomain of the VPAC1 receptor is a major site of vasoactive intestinal peptide (VIP) binding. Previous studies with the [Bpa6]-VIP and [Bpa22]-VIP probes (substitution with the photoactivable Bpa for the residues 6 and 22 in VIP) showed spatial approximation between the amino acids 6 and 22 of VIP and the 104-108 and 109-119 sequences within the N-terminal ectodomain of the receptor, respectively. Here, we characterize the new probe (Bz2-K24)-VIP (substitution with the photoreactive Bz2-K for the residue 24 in VIP). After photolabeling and sequential digestions of the receptor, the 121-133 sequence of the N-terminal ectodomain was identified as the site of interaction. The N-terminal ectodomain of the VPAC1 receptor is therefore an affinity trap for the central part of VIP, at least between residues 6 and 24.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Animals
  • CHO Cells
  • Cricetinae
  • Humans
  • Photoaffinity Labels / analysis*
  • Photoaffinity Labels / chemistry*
  • Receptors, Vasoactive Intestinal Polypeptide, Type I / metabolism
  • Vasoactive Intestinal Peptide / analysis
  • Vasoactive Intestinal Peptide / chemistry*
  • Vasoactive Intestinal Peptide / metabolism

Substances

  • (Bz2-K24)-vasoactive intestinal peptide
  • Photoaffinity Labels
  • Receptors, Vasoactive Intestinal Polypeptide, Type I
  • Vasoactive Intestinal Peptide
  • Adenylyl Cyclases