The fourth transmembrane segment forms the interface of the dopamine D2 receptor homodimer

J Biol Chem. 2003 Feb 14;278(7):4385-8. doi: 10.1074/jbc.C200679200. Epub 2002 Dec 19.

Abstract

Considerable evidence suggests that G-protein-coupled receptors form homomeric and heteromeric dimers in vivo. Unraveling the structural mechanism for cross-talk between receptors in a dimeric complex must start with the identification of the presently unknown dimer interface. Here, by using cysteine cross-linking, we identify the fourth transmembrane segment (TM4) as a symmetrical dimer interface in the dopamine D2 receptor. Cross-linking is unaffected by ligand binding, and ligand binding and receptor activation are unaffected by cross-linking, suggesting that the receptor is a constitutive dimer. The accessibility of adjacent residues in TM4, however, is affected by ligand binding, implying that the interface has functional significance.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Binding Sites / genetics
  • Cell Membrane / chemistry
  • Cell Membrane / metabolism
  • Cross-Linking Reagents
  • Cysteine
  • Humans
  • Ligands
  • Mutation
  • Receptors, Dopamine D2 / chemistry*
  • Receptors, Dopamine D2 / genetics
  • Receptors, Dopamine D2 / metabolism
  • Signal Transduction

Substances

  • Cross-Linking Reagents
  • Ligands
  • Receptors, Dopamine D2
  • Cysteine