Receptor-ligand interactions: binding affinities studied by single-molecule and super-resolution microscopy on intact cells

Chemphyschem. 2014 Mar 17;15(4):671-6. doi: 10.1002/cphc.201300755.

Abstract

Protein–ligand interactions play an important role in many biological processes. Notably, membrane receptors are the starting point for a huge variety of cellular signal transduction pathways. Quantifying the binding affinity of a ligand for its transmembrane receptor is of great importance as it provides information on the potency of the ligand. We developed a new experimental procedure to determine binding affinities of ligands for their membrane receptors directly on intact single cells using super-resolution imaging. Dissociation constants were determined by titrating fluorophore-labelled ligand against cells expressing the target protein and applying single-molecule imaging.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites
  • HeLa Cells
  • Humans
  • Ligands
  • Microscopy / methods*
  • Receptors, Cytoplasmic and Nuclear / chemistry*
  • Tumor Cells, Cultured

Substances

  • Ligands
  • Receptors, Cytoplasmic and Nuclear