Insights into the binding and activation sites of the receptors for cholecystokinin and gastrin

Magall Foucaud, Elodie Archer-Lahlou, Esther Marco, Irina G. Tikhonova, Bernard Maigret, Chantal Escrieut, Ingrid Langer, Daniel Fourmy

Research output: Contribution to journalLiterature review

32 Citations (Scopus)

Abstract

CCK receptors represent potential targets in a number of diseases. Knowledge of CCK receptor binding sites is a prerequisite for the understanding of the molecular basis for their ligand recognition, partial agonism, ligand-induced trafficking of signalling. In the current paper, we report studies from our laboratory and others which have provided new data on the molecularbasis of the pharmacology and functioning of CCK1 and CCK2 receptors. It has been shown that: 1) homologous regions of the two receptors are involved in the binding site of CCK, however, positioning of CCK slightly differs in agreement with distinct phannacophores of CCK toward the two receptors and receptor sequence variations; 2) Binding sites of most of non-peptide agonists/ antagonist are buried in the pocket formed by transmembrane helices and overlap that of CCK; Aromatic amino acids within and near the binding site, especially in helix VI, are involved in receptor activation; 4) Like for other members of family A of G-protein coupled receptors, residues of the binding sites as well as of conserved motifs such as E/DRY, NPXXY are crucial for receptor activation. (c) 2007 Elsevier B.V. All rights reserved.

Original languageEnglish
Pages (from-to)17-23
Number of pages7
JournalRegulatory Peptides
Volume145
Issue number1-3
DOIs
Publication statusPublished - 10 Jan 2008

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Neuroscience(all)

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