Packing density of the erythropoietin receptor transmembrane domain correlates with amplification of biological responses

Biochemistry. 2008 Nov 11;47(45):11771-82. doi: 10.1021/bi801425e. Epub 2008 Oct 15.

Abstract

The formation of signal-promoting dimeric or oligomeric receptor complexes at the cell surface is modulated by self-interaction of their transmembrane (TM) domains. To address the importance of TM domain packing density for receptor functionality, we examined a set of asparagine mutants in the TM domain of the erythropoietin receptor (EpoR). We identified EpoR-T242N as a receptor variant that is present at the cell surface similar to wild-type EpoR but lacks visible localization in vesicle-like structures and is impaired in efficient activation of specific signaling cascades. Analysis by a molecular modeling approach indicated an increased interhelical distance for the EpoR-T242N TM dimer. By employing the model, we designed additional mutants with increased or decreased packing volume and confirmed a correlation between packing volume and biological responsiveness. These results propose that the packing density of the TM domain provides a novel layer for fine-tuned regulation of signal transduction and cellular decisions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Asparagine / chemistry
  • Asparagine / genetics
  • Asparagine / metabolism
  • Binding Sites
  • Cell Line
  • Cell Membrane / metabolism*
  • Cell Proliferation
  • Dimerization
  • Flow Cytometry
  • Immunoblotting
  • Immunoprecipitation
  • Mice
  • Microscopy, Fluorescence
  • Mitogen-Activated Protein Kinase 1 / metabolism
  • Mitogen-Activated Protein Kinase 3 / metabolism
  • Mutation
  • NIH 3T3 Cells
  • Protein Structure, Tertiary
  • Proto-Oncogene Proteins c-akt / metabolism
  • Receptors, Erythropoietin / chemistry*
  • Receptors, Erythropoietin / genetics
  • Receptors, Erythropoietin / metabolism*
  • Signal Transduction / genetics
  • Signal Transduction / physiology

Substances

  • Receptors, Erythropoietin
  • Asparagine
  • Proto-Oncogene Proteins c-akt
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3