Rhodopsin activation exposes a key hydrophobic binding site for the transducin alpha-subunit C terminus

J Biol Chem. 2004 Jul 9;279(28):29767-73. doi: 10.1074/jbc.M402567200. Epub 2004 Apr 7.

Abstract

Conformational changes enable the photoreceptor rhodopsin to couple with and activate the G-protein transducin. Here we demonstrate a key interaction between these proteins occurs between the C terminus of the transducin alpha-subunit (G(Talpha)) and a hydrophobic cleft in the rhodopsin cytoplasmic face exposed during receptor activation. We mapped this interaction by labeling rhodopsin mutants with the fluorescent probe bimane and then assessed how binding of a peptide analogue of the G(Talpha) C terminus (containing a tryptophan quenching group) affected their fluorescence. From these and other assays, we conclude that the G(Talpha) C-terminal tail binds to the inner face of helix 6 in a retinal-linked manner. Further, we find that a "hydrophobic patch" comprising key residues in the exposed cleft is required for transducin binding/activation because it enhances the binding affinity for the G(Talpha) C-terminal tail, contributing up to 3 kcal/mol for this interaction. We speculate the hydrophobic interactions identified here may be important in other GPCR signaling systems, and our Trp/bimane fluorescence methodology may be generally useful for mapping sites of protein-protein interaction.

Publication types

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

MeSH terms

  • Animals
  • Binding Sites
  • Bridged Bicyclo Compounds, Heterocyclic / chemistry
  • Bridged Bicyclo Compounds, Heterocyclic / metabolism
  • COS Cells
  • Chlorocebus aethiops
  • Light
  • Models, Molecular
  • Molecular Structure
  • Mutation
  • Peptides / chemistry
  • Peptides / metabolism
  • Protein Conformation*
  • Protein Structure, Tertiary
  • Rhodopsin / chemistry*
  • Rhodopsin / genetics
  • Rhodopsin / metabolism*
  • Signal Transduction / physiology*
  • Transducin / chemistry*
  • Transducin / metabolism*

Substances

  • Bridged Bicyclo Compounds, Heterocyclic
  • Peptides
  • bimanes
  • Rhodopsin
  • Transducin