Antibodies binding the ADAM10 substrate recognition domain inhibit Eph function

J Cell Sci. 2012 Dec 15;125(Pt 24):6084-93. doi: 10.1242/jcs.112631. Epub 2012 Oct 29.

Abstract

The ADAM10 transmembrane metalloprotease cleaves a variety of cell surface proteins that are important in disease, including ligands for receptor tyrosine kinases of the erbB and Eph families. ADAM10-mediated cleavage of ephrins, the ligands for Eph receptors, is suggested to control Eph/ephrin-mediated cell-cell adhesion and segregation, important during normal developmental processes, and implicated in tumour neo-angiogenesis and metastasis. We previously identified a substrate-binding pocket in the ADAM10 C domain that binds the EphA/ephrin-A complex thereby regulating ephrin cleavage. We have now generated monoclonal antibodies specifically recognising this region of ADAM10, which inhibit ephrin cleavage and Eph/ephrin-mediated cell function, including ephrin-induced Eph receptor internalisation, phosphorylation and Eph-mediated cell segregation. Our studies confirm the important role of ADAM10 in cell-cell interactions mediated by both A- and B-type Eph receptors, and suggest antibodies against the ADAM10 substrate-recognition pocket as promising therapeutic agents, acting by inhibiting cleavage of ephrins and potentially other ADAM10 substrates.

Publication types

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

MeSH terms

  • ADAM Proteins / genetics
  • ADAM Proteins / immunology
  • ADAM Proteins / metabolism*
  • Animals
  • Antibodies, Monoclonal / genetics
  • Antibodies, Monoclonal / immunology
  • Antibodies, Monoclonal / metabolism*
  • Binding Sites, Antibody
  • Cattle
  • Cell Adhesion
  • Ephrins / metabolism*
  • HEK293 Cells
  • Humans
  • Mice
  • Protein Binding
  • Receptors, Eph Family / metabolism*
  • Signal Transduction

Substances

  • Antibodies, Monoclonal
  • Ephrins
  • Receptors, Eph Family
  • ADAM Proteins