Interaction of a fragment of the cannabinoid CB1 receptor C-terminus with arrestin-2

FEBS Lett. 2007 Oct 16;581(25):5009-16. doi: 10.1016/j.febslet.2007.09.030. Epub 2007 Sep 24.

Abstract

Desensitization of the cannabinoid CB1 receptor is mediated by the interaction with arrestin. In this study, we report the structural changes of a synthetic diphosphorylated peptide corresponding to residues 419-439 of the CB1 C-terminus upon binding to arrestin-2. This segment is pivotal to the desensitization of CB1. Using high-resolution proton NMR, we observe two helical segments in the bound peptide that are separated by the presence a glycine residue. The binding we observe is with a diphoshorylated peptide, whereas a previous study reported binding of a highly phosphorylated rhodopsin fragment to visual arrestin. The arrestin bound conformations of the peptides are compared.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Arrestins / chemistry*
  • Binding Sites
  • Humans
  • Models, Molecular
  • Molecular Sequence Data
  • Nuclear Magnetic Resonance, Biomolecular
  • Peptides / chemistry
  • Protein Structure, Secondary
  • Receptor, Cannabinoid, CB1 / chemistry*
  • beta-Arrestins

Substances

  • Arrestins
  • Peptides
  • Receptor, Cannabinoid, CB1
  • beta-Arrestins