Analysis of Interactions between the Epidermal Growth Factor Receptor and Soluble Ligands on the Basis of Single-Molecule Diffusivity in the Membrane of Living Cells

Angew Chem Int Ed Engl. 2015 Jun 8;54(24):7028-32. doi: 10.1002/anie.201500871. Epub 2015 May 4.

Abstract

We present a single-molecule diffusional-mobility-shift assay (smDIMSA) for analyzing the interactions between membrane and water-soluble proteins in the crowded membrane of living cells. We found that ligand-receptor interactions decreased the diffusional mobility of ErbB receptors and β-adrenergic receptors, as determined by single-particle tracking with super-resolution microscopy. The shift in diffusional mobility was sensitive to the size of the water-soluble binders that ranged from a few tens of kilodaltons to several hundred kilodaltons. This technique was used to quantitatively analyze the dissociation constant and the cooperativity of antibody interactions with the epidermal growth factor receptor and its mutants. smDIMSA enables the quantitative investigation of previously undetected ligand-receptor interactions in the intact membrane of living cells on the basis of the diffusivity of single-molecule membrane proteins without ligand labeling.

Keywords: cell membranes; diffusion; ligand-receptor interactions; super-resolution microscopy; transmembrane proteins.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal / immunology
  • COS Cells
  • Cell Membrane / metabolism
  • Cetuximab / immunology
  • Chlorocebus aethiops
  • Diffusion
  • ErbB Receptors / chemistry
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism*
  • Ligands*
  • Microscopy
  • Mutation

Substances

  • Antibodies, Monoclonal
  • Ligands
  • ErbB Receptors
  • Cetuximab