IADR Abstract Archives

Biophysical characterization of the pleiotrophin/RPTP zeta signaling mechanism

The receptor protein tyrosine phosphatase (RPTP βζ) and its extracellular ligand pleiotrophin (PTN or Osteoblast specific factor-1) have been shown to be involved in bone formation but have so far been mostly studied in the brain. Objectives: The long-term aims of our research are to determine the molecular mechanism with which PTN exerts its stimulatory effects of RPTPβζ in either bone or the brain. Three-dimensional structural understanding of this signaling system will open up for structure-based drug design of new PTN/RPTP small-molecule binding agents that might be able to treat osteoarthritis, osteopenia/osteoporosis, and other diseases associated with loss of or changes in bone density, in addition to a treatment for cancer.

The current signaling hypothesis is that PTN-induced/enforced dimerization of RPTPβζ results in loss of intracellular RPTPβζ phosphatase activity. In the absence of PTN signaling, RPTPβζ is shown to dephosphorylate beta-catenin (plus other important intracellular proteins), resulting in the normal formation of a β-catenin/E-cadherin molecular complex, which tethers actin filaments to the cell membrane. This is necessary for normal cell-cell adhesion. PTN signaling though the RPTPβζ receptor thus leads to decay of β-catenin/E-cadherin complex formation, due to loss of tyrosine dephosphorylation of β-catenin and disruption of the actin cytoskeleton and loss of cell-cell adhesion. Methods: We are using in vitro biophysical techniques (X-ray crystallography, calorimetry, Surface Plasmon Resonance) on the components of the entire signaling network of PTN/RPTPβζ to validate the current hypothesis.

Results: We have expressed PTN, and several individual domains of the RPTPβζ receptor in Escherichia coli. Biophysical characterization of these proteins is underway. Conclusions: It is possible to express and purify the extracellular PTN and RPTPβζ carbonic anhydrase and active phosphatase domains in E.coli, and this protein can now be used for X-ray crystallography and biophysical characterizations.


Division: IADR/CADR General Session
Meeting: 2008 IADR/CADR General Session (Toronto, Ontario, Canada)
Location: Toronto, Ontario, Canada
Year: 2008
Final Presentation ID: 2563
Abstract Category|Abstract Category(s): Mineralized Tissue
Authors
  • Erlandsen, Heidi  ( University of Alabama, Birmingham, AL, USA )
  • Johnson, Kenneth Alan  ( Centre for Biomolecular Sciences, SSPF, St. Andrews, N/A, Scotland )
  • SESSION INFORMATION
    Poster Session
    Bone Protein & Mineral
    07/04/2008