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Delineation of the peptide binding site of the human galanin receptor

Academic Article
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Overview

authors

  • Kask, K.
  • Berthold, M.
  • Kahl, U.
  • Nordvall, G.
  • Bartfai, Tamas

publication date

  • January 1996

journal

  • EMBO Journal  Journal

abstract

  • Galanin, a neuroendocrine peptide of 29 amino acids, binds to Gi/Go-coupled receptors to trigger cellular responses. To determine which amino acids of the recently cloned seven-transmembrane domain-type human galanin receptor are involved in the high-affinity binding of the endogenous peptide ligand, we performed a mutagenesis study. Mutation of the His264 or His267 of transmembrane domain VI to alanine, or of Phe282 of transmembrane domain VII to glycine, results in an apparent loss of galanin binding. The substitution of Glu271 to serine in the extracellular loop III of the receptor causes a 12-fold loss in affinity for galanin. We combined the mutagenesis results with data on the pharmacophores (Trp2, Tyr9) of galanin and with molecular modelling of the receptor using bacteriorhodopsin as a model. Based on these studies, we propose a binding site model for the endogenous peptide ligand in the galanin receptor where the N-terminus of galanin hydrogen bonds with Glu271 of the receptor, Trp2 of galanin interacts with the Zn2+ sensitive pair of His264 and His267 of transmembrane domain VI, and Tyr9 of galanin interacts with Phe282 of transmembrane domain VII, while the C-terminus of galanin is pointing towards the N-terminus of th

subject areas

  • Alanine
  • Amino Acid Sequence
  • Animals
  • Binding Sites
  • Cell Membrane
  • Cloning, Molecular
  • Conserved Sequence
  • DNA, Complementary
  • Galanin
  • Glycine
  • Histidine
  • Humans
  • Hydrogen Bonding
  • Kinetics
  • Ligands
  • Melanoma
  • Models, Molecular
  • Molecular Sequence Data
  • Mutagenesis, Site-Directed
  • Phenylalanine
  • Point Mutation
  • Polymerase Chain Reaction
  • Protein Structure, Secondary
  • Receptors, Galanin
  • Receptors, Gastrointestinal Hormone
  • Recombinant Proteins
  • Sequence Homology, Amino Acid
  • Swine
  • Tumor Cells, Cultured
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Research

keywords

  • galanin
  • ligand binding
  • molecular modelling
  • receptor
  • site-directed mutagenesis
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Identity

PubMed Central ID

  • PMC449938

International Standard Serial Number (ISSN)

  • 0261-4189

PubMed ID

  • 8617199
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Additional Document Info

start page

  • 236

end page

  • 244

volume

  • 15

issue

  • 2

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