ErbB1 dimerization is promoted by domain co-confinement and stabilized by ligand binding

Nat Struct Mol Biol. 2011 Oct 23;18(11):1244-9. doi: 10.1038/nsmb.2135.

Abstract

The extent to which ligand occupancy and dimerization contribute to erbB1 signaling is controversial. To examine this, we used two-color quantum-dot tracking for visualization of the homodimerization of human erbB1 and quantification of the dimer off-rate (k(off)) on living cells. Kinetic parameters were extracted using a three-state hidden Markov model to identify transition rates between free, co-confined and dimerized states. We report that dimers composed of two ligand-bound receptors are long-lived and their k(off) is independent of kinase activity. By comparison, unliganded dimers have a more than four times faster k(off). Transient co-confinement of receptors promotes repeated encounters and enhances dimer formation. Mobility decreases more than six times when ligand-bound receptors dimerize. Blockade of erbB1 kinase activity or disruption of actin networks results in faster diffusion of receptor dimers. These results implicate both signal propagation and the cortical cytoskeleton in reduced mobility of signaling-competent erbB1 dimers.

Publication types

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

MeSH terms

  • Cell Line, Tumor
  • Dimerization
  • ErbB Receptors / chemistry*
  • ErbB Receptors / metabolism
  • Humans
  • Ligands
  • Protein Binding
  • Protein Conformation*

Substances

  • Ligands
  • ErbB Receptors